Notes in Pharmacology - From Net

8/10/2019 Notes in Pharmacology - From Net

1/95

Monte laiza Eunice T.

DCB

PHARMACOLOGY - came from the Greek word "Pharmakon" which means "Drug" and "ogos" which means

"Discourse" ! "ogia" atin# - "$tud%". - it is a science that deals with the chemical and &h%sical &ro&erties of drugs' their sources'

effects' (iotransformation and e)cretion.

- it is the stud% of the effects of chemical su(stances u&on li*ing tissues.

HISTORY OF PHARMACOLOGY Pharmacologic thought had its (eginning when earl% humans (egan to wonder wh% the chewing of certain &lant roots or lea*es altered their awareness or functions. +s e)&erience in

root and leaf chewing &rogressed into thera&eutic (err% &icking and smoke smelling' the

e)&eriences were s&read and shared. +s time &rogressed' some indi*iduals (ecame more astute in o(ser*ing and remem(ering that &lant &roducts &roduced &redicta(le effects. Thus'

the first &harmacologist was (orn. Clearl% this hum(le (eginning has e*ol*ed through the

%ears into a huge industrial and academic communit% that is concerned with the stud% and

de*elo&ment of drugs. Drugs that e*ol*ed are then &rescri(ed and dis&ensed through the

&ractice of medicine' dentistr%' and &harmac%. for continuation - refer to ,olro%d#The histor% of &harmacolog% can (e di*ided into &eriods the earl% &eriod dates (ack to

anti/uit% and is characterized (% em&irical o(ser*ations in the use of crude drugs. 0t is interesting that e*en &rimiti*e &eo&le could disco*er relationshi&s (etween drugs and disease.

The use of drugs has (een so &re*alent throughout histor% that $ir 1illiam 2sler stated 3456#

with some 7ustification that man has an in(orn cra*ing for medicine. 0n contrast to this ancient &eriod' modern &harmacolog% is (ased on e)&erimental

in*estigations concerning the site and mode of action of drugs. The a&&lication of the

scientific method to studies on drugs was initiated in 8rance (% 8rancois Magendie and was

e)&anded (% Claude Bernard 3439-34:4#. The name of 2swald $chiemie De(ug 3494 353# is commonl% associated with the de*elo&ment of E)&erimental Pharmacolog% - in

German% and ;ohn ;aco( +(el 34


2/95


DCB

. Pharmaco!namics - deals with the effects of drugs in the (od%? deals with the mechanism

of action!effect of a drug in li*ing organisms and their corres&onding res&onses and the

&h%siologic and (iochemical effects of the drug. ",ow the drug &roduces its effect>" "1hat the drug does to the (od%>"

9. Pharmaco"nos! - identification and &rocurement of crude and naturall% occurring drugs.

8ormer name "Materia Medica"6. Pharmac! - &rocurement' &re&aration and dis&ensing of drugs.


3/95


DCB

(. Plants - crude drugs ma%(e o(tained from an% &art of *arious &lants used medicinall%.

E./ ea*es - Pito-&ito' +lagaw' Bana(a' etc.? digitalis from fo)glo*e &lant.

c. Minerals - iron' commonl% used in the form of ferrous sul&hate. $%nthetic!Chemical $u(stances - done in the la(orator% (% chemists.

a. Pure drugs and other sim&le su(stances

(. Products of com&le) s%nthesis anti(iotics' sulfonamides and adrenocorticosteroids#.

STAGES IN THE 'E-ELOPMENT OF A 'R+G

E*olution of a ew DrugDrug de*elo&ment $trategies

E)&erimental Pharmacolog%

To)icological +ssessment

Clinical E*aluationMarketing and Promotion

STRATEGIES

$erendi&it% luck and intuition# Molecular Foulette random clinical s%nthesis#

Program Basic Fesearch with $%nthesis of $&ecific Chemicals. Clinical 2(ser*ation of Drug +ction in the Practice.

PRINCIPAL IN'I-I'+AL.S/ STAGES IN THE 'E-ELOPMENT OF A 'R+G

CONCERNE'

arious 0deasChemist atural or s%nthetic chemical com&ounds

Pharmacologists Pharmacological Tests

Biochemists Performs "(iologic assa%s"To)icologists +cute to)icit% Chronic to)icit% tests

Mutagenicit% Teratogenesis Carcinogenecit%

Pharmacists Pharmaceutical formulation ! Clinical trialsClinical Pharmacologists Phase 3 + &ilot in*estigation made in a small num(er

ormal olunteers of normal *olunteers

Dentist!Doctor!Patients Phase +n o&en clinical trial carried out in a small

Clinical Pharmacologists num(er of &atientsurse Patients $tatistician Phase 9 arge scale clinical trial

Practicing Dentists!Doctors Phase 6 Monitored release and &ost- marketing

and their &atients sur*eillance of new drug +cce&ted drug

CLINICAL E-AL+ATION

Phase I

+ &ilot stud% that uses small num(ers of human *olunteers

0nitiall%' low doses of drug that are graduall% increased are used and the to)ic or e)aggerated

effects are monitored

Phase II

The drug is tested in limited num(ers of hos&italized &atients with the disease the drug is

0


4/95


DCB

intended to treat

The test drug is com&ared to esta(lished drugs and &lace(o

Phase III

Testing is intended to large grou& of out&atients to &ermit e*aluation of the drug under

conditions that ma% e)ist if the drug is marketed.

0f the drug is safe and effecti*e for its intended use' the 8D+ ma% a&&ro*e the drug for marketing.

Phase I-

+ new drug is usuall% marketed onl% after a few hundreds' or at most few thousand &atients ha*e (een e)&osed to it for a relati*el% short &eriod of time.

Post-marketing sur*eillance is necessar% to assess efficac% and to)icit% of a new drug on a

larger scale.

0 MA2OR PHASES IN A PRE3CLINICAL TESTS

3. +cute To)icit% Test

. $u(-acute &rolonged# To)icit% Test

9. Chronic To)icit% Test

PRINCIPLES OF 'R+G ACTION

3. Cure disease

. +lle*iate s%m&toms

9. Fe&lace deficiencies

F+N'AMENTAL ACTION OF 'R+GS

3. $T0M=+T02 - drugs that increases the o*erall acti*it% of s&ecialized organs' tissue' or cell.

e./. caffeine coffee - C$ stimulant? can cause tach%cardia inc. heart acti*it%#.. DEPFE$$02 - drugs that decreases the o*erall functional acti*it% of cells' tissues' or organs.

e./. alcohol' (ar(iturates.

9. 0FF0T+T02 - either inc. or dec. (ut it is said that stimulation is &ushed too far to the &oint of in7uring the cell.? manifested as nausea' *omiting' itchiness' redness.

6. FEP+CEMET ! $=PPEMET - drugs that can (e used as su(stitutes for what is lacking

in the (od%. e./. *itamins.


5/95


DCB

8or e)am&le' one drug drug +# &roduces com&lete eradication of &remature *entricular

contractions PCs# at a dose of 3 mg. + second drug drug B# &roduces com&lete

eradication of PCs at a dose of mg. Therefore' (oth drugs ha*e the same efficac% com&lete eradication of PCs#' (ut drug + is more &otent than drug B. 0t takes less of drug +

to &roduce the same effect. + third drug drug C# can reduce the PCs (% onl% AI' and it

takes a dose of


6/95


DCB

Gut Motilit%

Bronchoconstriction

icotinic Contraction of $triated Muscle

,0$T+M0E

,3 Bronchoconstriction Ca&illar% Dilation

, 0ncreased Gastric +cid

D2P+M0E C$ eurotransmitter

2P02D C$ eurotransmitter

00. +CT02 2 EJHME

Enz%me - &rotein macromolecule with which su(stances interact to &roduce Kacti*ationL

or Kinhi(itionL.

Drugs in clinical use which e)ert their effect thru enz%me action generall% do so (% Kinhi(itionL.

E./. +s&irin inhi(its &latelet c%clo-o)%genase? +llo&urinol inhi(its )anthene o)idase.

000. +CT02 2 MEMBF+E 020C C,+E$

The conduction of im&ulse in ner*e tissues and electrochemical cou&ling in muscles de&ends on the mo*ement of ions &articularl% sodium' calcium' and &otasium through

mem(rane channels.

$e*eral grou& of drugs that interfere with these &rocessess +ntiarr%thmic drugs'

General and local anesthesia' +nticon*ulsant.

0. CHT2T20C +CT02$

This mechanism ha*e (een defined in terms of effects on s&ecific rece&tors or enz%mes.But in other cases' chemical action +lk%lation# damages D+ or other macromolecules

and results in cell death or failure of cell di*ision.

E./. Drugs used in cancer or in treatment of infection ma% kill malignant cells or Microorganisms.

P+BLICATIONS IN PHARMACOLOGY

+&S&P& +nite States Pharmaco%oeia

-

Fe&resentati*es from school of medicine and &harmac%- +merican medical +ssociation- +merican Pharmaceutical +ssociation

- $tate Medical $ocieties

- +merican Chemical $ociet%- 2ther scientific organization and federal agencies

Pur&ose of =.$.P. 0t sets the official chemical and &h%sical standards that relate

essentiall% to strength and &urit% of drug.

7


7/95


DCB

N&F& Nationa# Form)#ar!

- issued e*er% < %ears

- esta(lishes official standards for drugs not descri(ed in the =.$.P. - descri(ed e)tent of drugs use and thera&eutic *alue

British Pharmaco%oeia - English e/ui*alent of =.$.P. Great Britain and Canada#

Pharmaco%oeia Internationa#is

- issued (% 1.,.2.

A&'&T& Acce%te 'enta# Thera%e)tics

A&'&R& Acce%te 'enta# Remeies

- (iennial &u(lication of the Council on Dental Thera&eutics CDT# of the +merican Dental

+ssociation

- drugs of recognized *alue that are la(eled and ad*ertised in accordance with CDT are

included. - Primaril% a hand(ook of dental &harmacothera&eutics and intended to assist the dental

&ractitioner in the selection of drugs.

P&'&R& Ph!sician8s 'esk Re4erence

- a hand(ook &u(lished annuall% (% some manufacturers

Special Value: 3. Pu(lished annuall% and therefore includes relati*el% u& to date information

. 0t is cross-inde)ed to include the use of &ro&rietar% names

Disadvantages: 3. Products or drugs are arranged (% manufacturers rather than (% &harmacologic class

. 0nformation ma% (e "(iased".

REP+BLIC ACT 7796 - known as the GENERIC ACT OF 1:;; - an act to Promote' Fe/uire and Ensure the &roduction of an ade/uate su&&l%'

distri(ution' use and acce&tance of drugs and medicines identified (% their generic names.

+0M3. To &romote' encourage and re/uire the use of generic terminolog% in the im&ortation'

manufacturing' distri(ution' marketing' ad*ertising and &romotion' &rescri&tion and

dis&ensing of drugs.

. To ensure the ade/uate su&&l% of drug with generic names through a rational s%stem of &rocurement and distri(ution.

9. To encourage the e)tensi*e use of drug with generic names through a national s%stem of

&rocurement and distri(ution.

Importance of R.A. 6675

3. 8or health &rofessionals to (ecome more aware and cognizant of their thera&eutic effecti*eness.. To &ro*ide drugs to indigent &atients at the lowest &ossi(le cost.

9. To ha*e health% com&etition among drug manufacturers

9


8/95


DCB

Who Shall se !eneric "erms#

+ll go*ernment health agencies

+ll medical' Dental and eterinar% &ractitioners+ll drug esta(lishments

+ll drug outlets

Pena#t! 4or NOT com%#!in" to R&A& 7796

$irst %ffense

Fe&rimand which will (e recorded in the Professional Fegulation Commission Book.Second %ffense

8ine ot less than P'. (ut not greater than P


9/95


DCB

+d*antages of Trade ames

3. The% are con*enient and sa*es time when writing &rescri&tions for multi&le-entit% drugs

. Trade names are usuall% shorter and easier to remem(er than generic names.9. The use of trade names demands the &roduct of a s&ecific manufacturer in whose

manufacturing &ractices the &ractitioner ma% ha*e s&ecial confidence.

0& GENERIC NAME - "2fficial" name of the drug? "on-Pro&rietar% name.

+d*antages of using Generic ames3. ,ealth% com&etition among drug manufacturers

. Pro*ides a wide selection of drugs

9. 0t is uni*ersall% acce&ted.

Disad*antages of using Generic ames

3. ot all &re&arations are &re&ared as the% should (e.

. 0t is hard to remem(er.

9. 0t is incon*enient when written.

E.g.

Chemica# -dieth%lamino 'A aceto)%lidide -acet%l &-amino&henol

Generic idocaine +cetamino&hen

Trae Name %locaine T%lenol Dolicaine Tem&ra

2ctocaine aladol

-caine Datril

Ho< to )se the PIMS = MIMS

PIMS - Phili&&ine 0nde) for Medical $&ecialties

MIMS- Monthl% 0nde) for Medical $&ecialties. 0t is a glo(al term for a thera&eutic inde).

Brand ame !Manufacturer ! Distri(utor Contents C #

0ndication!s 0 #

Dosage D #

Contraindications C!0 # $&ecial Precautions $P #

+d*erse Feactions +F #

Drug 0nteractions D0 # Presentation ! Price P!P #

&'ample: Based from M0M$ Dental Phils. &age A4#

ATMOSE Morishita-$eggs F) +tmose is the &ro&rietar% name of the

Metro Drug# drug?

C& Mefenamic +cid Morishita-$eggs is the name of the

I& Felief of mild to moderate &ain including com&an% who manufactured the drug

:


10/95


DCB

headache' dental &ain' &ost-o& and &ost&artum Metro Drug is the name of the

&ain' d%smenorrhea' osteoarthritis and F+. com&an% marketing the &roduct

'& +dult and children N 36 %r. 0nitiall%


11/95


DCB

9. Cough and Cold Femedies

6. Decongestants and other asal Pre&arations


12/95


DCB

-III& OTHER CHEMOTHERAPE+TICS

3. +ntitu(erculous +gents. $ul&honamides

9. +ntiamoe(ics

6. +nthelmintics


13/95


DCB

>III& EYE EAR MO+TH = THROAT

EHE3. E%e +nti-infecti*es and +ntise&tics

. E%e corticosteroids

9. E%e +ntise&tics with Corticosteroids6. M%driatic Drugs

I-& 'ERMATOLOGICALS

3. To&ical +nti-infecti*es

. To&ical +nti-infecti*es with Corticosteroids9. To&ical Corticosteroids

6. +cne Treatment Pre&arations

-II& ALLERGY AN' IMM+NE SYSTEM

3. +ntihistamines and +ntiallergies. accines' +ntisera and 0mmunologicals

9. 0mmunosu&&ressants

10


14/95


DCB

>-III& ANTI'OTES AN' 'ETO>IFYING AGENTS

>I>& INTRA-ENO+S AN' OTHER STERILE SOL+TIONS

>>& MISCELLANEO+S

'i44erent Factors A44ectin" Res%onse

Foutes of Drug +dministration Passage of Drug +cross Bod% Mem(ranes

Molecular Mechanism of +ction

+(sor&tion Distri(ution 8+TE of a DF=G

Meta(olism

E)cretion

RO+TES OF 'R+G A'MINISTRATION

ENTERAL

2ral

Fectal

PARENTERAL

()podermic Routes

0ntra*enous 0ntramuscular

$u(cutaneous

0ntradermal 0ntrathecal

0ntra&eritoneal

Additional Routes To&ical

0nhalation

$u(lingual Transdermal

LOCAL RO+TE

To&ical 0ntradermal

0ntrathecal 0ntranasal

0ntracon7ucti*al

0ntra-oral

0ntra-articular 0ntra-arterial

2ther s&ecial routes

15


15/95


DCB

SYSTEMIC RO+TES

Enteral

Parenteral

*** +ocall) administered drugs ma) ,e a,sor,ed at a rate and to an e'tent sufficient to result in

the production of s)stemic effects.

ENTERAL RO+TES- drug is &laced directl% into the G0T from where a(sor&tion occurs.

A& ORAL RO+TE

- sim&lest and most con*enient for self administration.

Contraindication for 2ral Foute

3. Patients with gastrointestinal intolerance . Patients &re&aring for anesthesia

9. Patients with gastrointestinal surger%

6. Precluded in coma

Disad*antages of 2ral Foute

3. 0rritant drugs cannot alwa%s (e gi*en (% mouth for it ma% cause sickness.. 0t is not feasi(le to gi*e drugs (% this route to &atients who are *omiting or mori(und.

9. Man% drugs are destro%ed (% the action of the digesti*e ferments (efore the% can (e

a(sor(ed.6. 0ntestinal a(sor&tion ma% (e irregular due to other su(stances in the git.


16/95


DCB

Pethidine

Fes&irator% Drugs

$al(utamol Ter(utaline

Drugs +cting on Central er*ous $%stem

Chlormethiazole Chlor&romazine

0mi&ramine

e*odo&a ortri&t%line

2ral Contrace&ti*es

Cardio*ascular Drugs

Gl%cer%l Trinitrate 0so&renaline

ifedi&ine

Prazosin

Pro&anolol era&amil

ignocaine Metro&olol

RECTAL RO+TE

- drugs are given via the rectum. &.. solid form / suppositories0 liuid form / enemata. - used when oral administration is im&ossi(le.

- avoids the acidit) and en1)mes of the gastric 2uice and first pass meta,olism.

- Both local and s%stemic effects are o(tained (ut a(sor&tion of man% drugs are oftenirregular and incom&lete. 0ndications Pediatrics ! Geriatrics

PARENTERAL RO+TES - generall% chosen when s&eed or relia(ilit% are s&eciall% desired.+. 0n7ection R essential if the drug is to (e a(sor(ed in acti*e form.

- a(sor&tion is usuall% more &redicta(le and more ra&id

- re/uires s&ecial skill? drugs cannot (e withdrawn easil%.

Disadvantages

3. Difficult for the &atients to &erform the in7ection (% themsel*es.

. $trict ase&sis must (e maintained to a*oid infection

9. =suall% more costl% and less safe.6. Can cause &ain.

TYPES OF IN2ECTION

Intra(eno)s .I-/

- route of choice for emergenc% cases - Most ra&id route ! method to elicit drug res&onse.

+d*antages

3. Fa&id action

. Can (e used for drugs which are irritant (% 0M in7ection.9. =seful for ill' hos&italized &atients when a slow 0 infusion &ro*ides a stead% flow

without distur(ing the &atient

17


17/95


DCB

Disad*antages

3. Tend to &roduce more immediate ad*erse reactions.

. Too high concentration of the drug is readil% o(tained when in7ected ra&idl%.9. The chance of &enetration into an arter% instead of a *ein is a &ossi(ilit%.

Com&lications 3. Drug $hock

. +cute' serious' allergic res&onses

9. Phle(itis 6. ecrosis around the in7ection site.

Intraerma# .c)taneo)s/- E./. skin testing.

+ction

- local effect

- small amount is in7ected into the e&idermis of the skin so that *olume does not interfere

with wheal formation or cause a s%stemic reaction.- used for o(ser*ation of an inflammator% allergic# reaction to foreign &roteins.

- rarel% em&lo%ed e)ce&t in certain Diagnostic and test &rocedures screening forallergic or local irritant res&onses#.

- takes the longest time for drug a(sor&tion.

$ites

- ocations are chosen so that inflammator% reaction can (e o(ser*ed. Preferred areas

are lightl% &igmented' thinl% keratinized' and hairless such as *entral mid-forearm'

cla*icular area of chest' sca&ula area of (ack' and medial as&ect of thighs.

E/ui&ment

eedle A R : gauge $%ringe 3 ml. cali(rated in .3 ml. increments

=suall% .3 R .3 ml. in7ected.

Techni/ue

Cleanse area using circular motion? o(ser*e sterile techni/ue.

,old skin taut.

0nsert needle' (e*el u&' at a 3< degree angle? outline of needle under the skin should (e *isi(le.

0n7ect medication slowl% to form a wheal (lister or (le(#.

Femo*e needle slowl%. Make a mark or encircle the (le( with a &en.

Do not massage area? instruct client not to do so.

+ssess for allergic reaction in 6 R : hours? measure diameter of local reaction.

S)?c)taneo)s - for drugs which are not irritant to tissues. E./. mor&hine sul&hate'

adrenaline' and insulin.

- *olume is usuall% 3 ml. or less? seldom e)ceeds ml. - cutaneous (lood flow is slower com&ared to 0M

- sustained effect can (e o(tained (% &lacing a &ellet of drug su(cutaneousl%? e./.

19


18/95


DCB

Estradiol &lants.

- drug is in7ected in the su(cutaneous la%er into the al*eolar connecti*e tissue 7ust (elow the

skin.

+ction

-

$%stemic effect- $ustained effect? a(sor(ed mainl% through ca&illaries? usuall% slower in onset than with

intramuscular route.

- =sed for small doses of non-irritating water-solu(le drugs.

$ites

- ocations for su(cutaneous in7ection are chosen for ade/uate fat &ad size and include the

a(domen' u&&er hi&s' u&&er (ack' lateral u&&er arms' and lateral hi&s.

E/ui&ment

eedle < R : gauge

S -

=suall% .< R 3.< ml. in7ected. 0nsulin s%ringe measured in units for use with insulin onl%.

Techni/ue Cleanse area with circular motion using sterile techni/ue

Pinch the skin.

0nsert needle at angle a&&ro&riate to (od% size. 6< to 5 degrees.

Felease skin. +s&irate' e)ce&t with he&arin.

0n7ect medication slowl%.

Femo*e needle /uickl%. Gentl% massage area' unless contraindicated with he&arin.

+&&l% &laster if needed.

+d*antages

3. $&read the action out o*er a num(er of hours.

. +*oid too intense or too short res&onse

9. +*oid fre/uent in7ections.

+a)er of s3in and site of in2ections:

E&idermis

Cutaneous Dermis

Mem(rane

8ascia

$u(cutaneous Muscle

1;


19/95


DCB

Intram)sc)#ar .IM/

- more dangerous than 0? (etter for irritant tissues.

+ction

- s%stemic effect.

-

=suall% more ra&id effect of drug than with su(cutaneous.- =sed for irritating drugs' a/ueous sus&ensions' and solutions in oils.

- indicated when an immediate effect is not re/uired (ut a &rom&t effect is desira(le.- 3 R

9 minutes a(sor&tion.

$ites

ocations are chosen for ade/uate muscle size and minimal ma7or ner*es and (lood

*essels in the area. Preferred locations include *entrogluteal' dorsogluteal' deltoid' and*astus lateralis.

E/ui&ment

eedle 34 R 3 gauge 3 R 3.< in. in length

$%ringe 3 R9 ml. =suall% .< R 3.< ml. in7ected

Techni/ue $ame as for su(cutaneous in7ection e)ce&t that needle is inserted at 5 degree angle into

the muscle.

Fi")re +ngles for in7ections. +# 0M 5 B# C# D# $C 5 ' A ' 6< E# 0D 3@3< .

Intra%eritonea#R in7ected into the &eritoneal ca*it% (% a(sor&tion of messenteric *eins

Intra%#e)ra# - introduce into the &leural ca*it%? for as&iration of fluids.

1:


20/95


DCB

Intratheca# = Intras%ina# - for s&inal analgesia into the s&inal su(arachnoid s&ace.

- administered into the cere(ros&inal fluid at an% le*el of the cere(ros&inal a)is.

Intrane)ra# - used in trigeminal neuralgia.

Intrasterna# - drugs which normall% do not cross the (lood (rain (arrier.

B+CCAL an S+BLING+AL ro)te

- an enteral route infre/uentl% used (ut useful in drugs with first &ass he&atic meta(olism.E./. gl%cer%l trinitrate for angina attack (ut ineffecti*e when swallowed as its first &ass

meta(olism a&&roaches 3 &er cent

- drugs that are susce&ti(le to degradation (% the G0T and e*en the li*er are safel%

administered su(linguall%.

INHALATION - E./. inhalation anesthetics' aerosol inhalation for asthma.

- inhalation is *ia the mouth? a(sor&tion occurs in the small (ronchioles. E./. disodium

cromogl%cate *ia a K$&inhalerL.- drug is a(sor(ed through the &ulmonar% endothelium at the al*eoli to gain ra&id access

to the general circulation.

Feasons for ra&id a(sor&tion

3. +l*eolar and *ascular e&ithelial mem(ranes of the lungs are /uite &ermea(le.. Blood flow is a(undant.

9. There is al large surface for a(sor&tion.

Particle $ize3. Particles greater than 0 um in diameter - tend to settle in the (ronchi.

. Particles less than .< um - fail to settle? mainl% are e)haled.

TOPICAL

- least effecti*e.

- drug is a&&lied to the skin and other e&ithelial surfaces with glo*e' tongue (lade' orcotton-ti&&ed a&&licator.

- utilized for local drug effect.

- =se a&&ro&riate techni/ue to remo*e medication form container and a&&l% to clean' dr%

skin' when &ossi(le. Do not contaminate medication in container' use glo*es or ana&&licator.

Methods of enhancing drug a(sor&tion *ia the To&ical route3. 0onoto&hresis - uses gal*anic current

. 0nunction - mechanical ru((ing of drug into the skin.

TRANS'ERMAL

- stored in a &atch &laced on the skin and a(sor(ed through skin' ha*ing s%stemic effect

- Transdermal drugs &ro*ide more consistent (lood le*els and a*oid G0 a(sor&tion

associated with oral &roducts.

,@


21/95


22/95


23/95


DCB

in all res&ects to the re/uirements for in7ections 9# $olids sus&ended in a suita(le

fluid medium which are not to (e in7ected 0 or into the s&inal canal 6# dr% solids'

which u&on the addition of suita(le *ehicles' %ield &re&arations conforming to the re/uirements for sterile sus&ensions and


24/95


DCB

=nits Meter m# @ for length

iter l# @ for ca&acit%

Gram gm.# @ for weight

Metric Ta?#es

Ta?#e o4 Len"th Ta?#e o4 Ca%acit! Ta?#e o4 ei"ht3 km. @ 3' m. 3 kl. @ 3' l. 3 kg. @ 3' gm.

3 hm. @ 3 m. 3 hl. @ 3 l. 3 hg. @ 3 gm.

3 dkm @ 3 m. 3 dkl @ 3 l. 3 dkg @ 3 gm.3 dm. @ .3 m. 3 dl. @ .3 l. 3 dg. @ .3 gm.

3 cm. @ .3 m. 3 cl. @ .3 l. 3 cg. @ .3 gm.

3mm. @ .3 m. 3ml. @ .3 l. 3mg. @ .3 gm.

Proce)re 4or Con(ersion Bet gm.

3 mg. 3 gm. @ A6 mg. ) gm. 3 ) @ A6

) @ . A6 .

3

@ .A6 gm.

(. 9< ml. @ >

3 ml. 3. @ 9< ml. ) .

3 ) @ 9< ) @ .9< .

3

@ .9<

II& APOTHECARIES OR ENGLISH SYSTEM - 0n this older s%stem' Foman numerals

and common fractions are used to designate units. +lso' the units of measure &recede the numeral in correct form. e./ the correct wa% to signif% grains would (e Kgr.)).L +

line is often written a(o*e the numerals' and a dot is &laced a(o*e the numeral 0 to

distinguish more clearl% (etween the two 0Os and a or hastil% written. 1hen using the a&othecar% s%stem in calculations' howe*er' the +ra(ic num(ers are used.

Procedure for Con*ersion 1ithin the a&othecar% $%stem

3. 1rite the e/ui*alent (etween the terms to (e con*erted as the first two terms of the&ro&ortion.

,5


25/95


DCB

. Being careful to kee& the units in the last two terms in the same order as the% occur

in the first' write the known /uantit% and the unknown e/ui*alent as the third and

fourth terms of the &ro&ortion. E)am&les

a. A drams @ > ounces

4 drams 3 ounce @ A drams ounces4 ) @ A

) @ .A . @ . 9 . ounce4 6

(. drams @ > minims

A minims 3 dram @ ) minims drams

3 ) @ 3

) @ 3 minims

T+BE 28 1E0G,TA grains @ 3 dram

4 drams @ 3 ounce 3 ounces @ 3 l(.

T+BE 28 C+P+C0TH A minims @ 3 fluidram

64 minims or 4 fluidrams @ 3 fluid ounce

:A4 minims or 3A fluid ounces @ 3 &int

&ints @ 3 /uart 6 /uarts @ 3 gallon

III& HO+SEHOL' SYSTEM 3 The household s%stem of measurement is not as accurate as the metric s%stem (ecause of the lack of standardization of s&oons' cu&s' and glasses.

The measurements are a&&ro)imate.

,2=$E,2D =0T$ 28 ME+$=FEMET

A dro&s gtt# @ 3 teas&oon

9 teas&oon @ 3 ta(les&oon t(s#

A teas&oon @ 3 ounce t(s @ 3 oz.

A oz. @ 3 tea cu&

4 oz. @ 3 glass 4 oz. @ 3 measuring cu&

2T,EF E=0+ET$ 3' cc. @ 3 @ 3 /uart


26/95


DCB

6 gms. @ 3 dram @ A grains

TEMPEF+T=FE C2EF$02 Celsius to 8arenheit C # 5!METRIC 'OSES IMATE APOTHECARY E+I-ALENTS

(% Musser!2Oeil re&rinted from =$P 0#

LI+I' MEAS+RE

A%%ro$imate

METRIC APOTHECARY

e)i(a#ents

A%%ro$imate

METRIC APOTHECARY

e)i(a#ents

3 ml. 3 /uart 9 ml. 6< minims

:


27/95


DCB

.6 Gm. A grains 3 mg. 3!A grain

.9 Gm. < grains .4 mg. 3!4 grain

.< Gm. 6 grains .A mg. 3!3 grain

. Gm. 9 grains .< mg. 3!3 grain

.3< Gm. S grains .6 mg. 3!3


28/95


DCB

Fries R)#e

- sometimes used in calculating dosages for infants less than %ears old.

+ge mos.# +dult dose

--------------------------------- @ 0nfant dose

3AKOLE/

=sual Dose 0' C, - 4 mg. TMP and 6 mg. $M!kg.!d di*./3h P2

+dults - 9 mg. TMP and 3A $M!d di*./3h P2 Pre&arations 2ral - 3' units!ml. 9 ml. sus&ension?


37/95


DCB

DETOCONAKOLE

=sual Dose C, -


38/95


DCB

Drugs ma) ,e com,ined in prescriptions for the follo8ing reasons:

3. To o(tain the con7oint effect of two or more acti*e su(stances.

. To diminish or annul undesira(le effects &roduced (% one or more of the acti*eingredients.

9. To increase the solu(ilit% or aid in the dis&ensing of the acti*e su(stances.

6. 2ccasionall%' to &roduce a new com&ound.

PARTS OF AN I'EAL PRESCRIPTION

WWWWWWWWDoctorOs ameWWWWWWWWWWWWWWWWWWWWWW+ddressWWWWWWWWWWWWWW

WWWWWWWWTel. o.WWWWWWWW

----------------------------------------------------------------------------------------------------------------------

PatientOs name WWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWW DateWWWWWWWWWWWWW

+ddressWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWWTel. o. WWWWWWWWWWWWWWWWWW +ge WWWWWW $e) WWWWWW

R$

Generic name of drug' dosage form and amount .

Brand name of drug#

Direction to the &harmacist .

Direction to the &atient .

WWWWWWWWWWWWWWWWWW D.M.D. Prescri(erOs $ignature

PFC icense um(er

P.T.F. um(er .

arcotic icense um(er $-#

T.0.. Ta) 0dentification um(er

WWWWWWWWWWWWWWWWWWWW Refill Information

0;


39/95


DCB

Parts o4 the Prescri%tion

S)%erscri%tion PatientOs name' address' and age? date and the s%m(ol F).

Inscri%tion ame of drug' dosage form' and amount. S)?scri%tion Directions to the &harmacist

Transcri%tion = Si"nat)re Direction to the &atient

HEA'ING

ame' address and &hone num(er of the &rescri(er.

ame' address' age' and &hone num(er of the &atient' and date

BO'Y

The s%m(ol F)

ame and dosage unit or concentration li/uids# of the drug. +mount to (e dis&ensed

Directions to the &atient

CLOSING Prescri(erOs signature

$&ace for DE+ num(er Fefill instructions

KPlease &lace name of drug on la(elL

0m&ortance of &lacing the name of the drug on la(el

3. 0n case of o*erdose or ad*erse reactions' the drugsO identit% can (e /uickl% o(tained.

. 2ther &ractitioners can identif% drugs the &atient is taking.

9. 0n most cases' the &atient has the right to know what drug he or she is taking.

,ints for Prescri&tion 1riting

3. 1rite legi(l% in ink or ha*e it t%&ewritten. =se the metric s%stem

9. +*oid a((re*iations

6. Qee& a co&% of each &rescri&tion or transcri(e the information to the &atientOs record.


40/95


DCB

Considerations in Drug +dministration ! Prescri(ing

3. Tolerance R the a(ilit% of a client to res&ond to a &articular dose of a certain drug ma%

diminish after da%s or weeks of re&eated administration. + com(ination of drugs ma% (egi*en to decrease or dela% the de*elo&ment of tolerance for a s&ecific drug.

. Pathologic $tate ! Pre-e)isting Disease $tate - i*er' kidne%' heart' circulator% and

gastrointestinal disorders are e)am&les of &ree)isting states that can affect a res&onse to adrug. 8or instance' dia(etics should not (e gi*en eli)irs or s%ru&s than contain sugar.

9. +ge - The age of a &atient will affect his or her res&onse to drugs. Children and elderl%

&ersons are more sensiti*e to drugs? the% re/uire less than the usual adult dose.6. 1eight - the more a &erson weighs' the more dilute the drug will (ecome and a smaller

amount will accumulate in the tissues. 2n the other hand' the less a &erson weighs' the

greater accumulation in the tissues and a more &owerful drug effect is &roduced.


41/95


DCB

LATIN PHRASES an ABBRE-IATIONS

+ se in PRESCRIPTION RITING

A??re(iations L a t i n E n " # i s h

a. ante (efore

aa ana of each

a.c. ante ci(um (efore meals

ad ad to' u& toass. adde' addantur add' let them (e added

ad li(. ad li(itum at &leasure

ac/. ac/ualis e/ual

agit. agita shake

a/. a/ua water

a/. dest. a/ua distilata distilled water

am&. --- am&ule

(. (is twice

(ene (ene well

(.i.d. (is in die twice a da%

c ci(um meal

c. cum with

ca&. ca&sula ca&sule

co. ? com&. com&ositus com&ound

coch. mag. cochleare magnum a ta(les&oonful

coch. med. cochleare medium a desserts&oonful

coch. &ar*. cochleare &ar*um a teas&oonful

cong. congium a gallon

d. dies a da%

da da gi*e

d. in &. ac/. di*idatur in &artes ac/uales let it (e di*ided into e/ual &artsd.t.d. dentus tales doses gi*e such doses

die( alt. die(us alternis e*er% other da%

dil dilitus dilute

dis&. dis&ensa' dis&ensetur dis&ense

di*. di*ide di*ide

dos. dosis a dose

E.C. --- enteric coated

eli). eli)ir eli)ir

Et et and

E) e) out of

E)t e)tractum e)tract

e) a/. e) a/ua with water

e.m.&. e) modo &rescri&to after the manner &rescri(ed

f. fiat' fiant make' let (e made

8ac face make

fl. or fld. fluidus fluid

8t. fiat make

gm. --- gram

gr. --- grain

gtt. gutta' guttae a dro&' dro&s

h hora hour h.s. hora somni at (edtimehour of slee

---

51


42/95


DCB

'R+G THERAPY

Pharmace)tica# Process

Pharmacokinetics Process

Pharmaco!namics Process

Thera%e)tic Process

PHARMACE+TICAL PROCESS

Is the drug getting into the patient# +&&ro)imatel% 4I of drugs are taken (% mouth? therefore' the &harmaceutic &hase is the

first &hase of drug action. 0n the gastrointestinal tract' drugs need to (e in solution to (e

a(sor(ed. + drug in solid form ta(let or &ill# must disintegrate into smaller &articles in order for it to dissol*e into a li/uid.

'isinte"rationis the (reakdown of the ta(let or &ill into smaller &articles.

'isso#)tionis the dissol*ing of smaller &articles in gastrointestinal fluid for a(sor&tion.

Rate Limitin"is the time it takes for the drug to disintegrate and (ecome a*aila(le for the (od% to a(sor( it.

8actors to consider

3. Particle size - the smaller the &article size' the faster it can (e a(sor(ed in the (od%.

. E)ci&ients of drug - fillers and inert su(stances are used in drug &re&aration to allow thedrug to take on a &articular size and sha&e and to enhance dissolution of the drug. $ome

additi*es such as Q and a in &enicillin Q and &enicillin a' increase the a(sor(a(ilit% of

the drug.

9. Coating material - Enteric-coated EC# drugs resist disintegration in the gastric acid inthe stomach' so disintegration does not occur until the drug reaches the alkaline

en*ironment in the small intestine.

PHARMACODINETIC PROCESS

Is the drug getting into its site of action#

- is the &rocess of drug mo*ement to achie*e drug action.- concerned with the a?sor%tion istri?)tion an e#imination .meta?o#ism an e$cretion/

of drugs.

ABSORPTION

- &rocess (% which drug molecules are transferred form the site of administration in the (od%

to the circulating fluids

8actors +ffecting +(sor&tion

3. Ph%sico-chemical factors

. $ite of a(sor&tion ! Blood flow at the site 9. Drug $olu(ilit%

6. Effects of food

a. Blood flow (. Gastric em&t%ing

5,


43/95


DCB

the non-ionized &ortion (eha*es as a non-&olar li&id solu(le com&ound which readil%

tra*erses (od% mem(ranes.

The amount of ionization that an% weak electrol%tes undergoes de&end on the &, at the

drug site in the tissues and its dissociation characteristics.

0ncrease &, weak acids# - the greater the degree of ionization

Decrease &, weak (ases# R the greater the degree of ionization.

2ral a(sor&tion R de&ends on the dosage form of drugs.

+(sor&tion on in7ection sites - de&ends on the solu(ilit% of drug and the (lood flow at the

site? also affected (% dosage form. E./. drugs in sus&ension are a(sor(ed much ore slowl% than those in solution.

Effects of food on drug a(sor&tion - (% affecting the (lood flow and gastric em&t%ing. E./. li/uid glucose meal decreases

flow and a meal rich in &rotein increases flow.

- some drugs are irritating to the stomach mucosa' so fluids or food are necessar% to

dilute drug concentration - there are drugs that are a(sor(ed easil% in the &resence of food.

8actors that Modif% the Fate of +(sor&tion3. Drug Concentration at the $ite

. Circulation to the $ite of +(sor&tion

9. +rea of +(sor&ti*e surface

FACTORS GO-ERNING THE FATE OF A 'R+G

1& Mo#ec)#ar ei"ht

- su(stances with high molecular weight are not usuall% a(sor(ed intact e)ce&t in minute

/uantities. - the% are a(sor(ed (% enz%matic actions. E./. insulin is a &rotein R it undergoes

enz%matic (reakdown in the git and is not a(sor(ed.

,& Chemica# Sta?i#it!

- unsta(le drugs ma%(e inacti*ated in the git. E./. Benz%l&enicillin in unsta(le in acid

medium and cannot (e effecti*e if gi*en (% mouth. Pheno)%meth%l&enicillin is more sta(le in acid medium.

0& Li%i So#)?i#it!

- if the drug is li&id solu(le' it can easil% &ass through the mem(rane.

5& 'e"ree o4 Ioniation

- the unionized &ortion of a drug is li&id solu(le and so is readil% a(sor(ed? ionized

&ortion is li&id insolu(le.

THE CELL MEMBRANE

Com&osition

i&ids 6I# &hos&holi&ids - makes mem(rane relati*el% im&ermea(le to ions and &olar molecules

Proteins


44/95


DCB

Car(oh%drates remainder# 2ligosaccharide

- linked co*alentl% to form com&le)es of gl%co&roteins and gl%coli&ids

PRINCIPAL MECHANISMS IN-OL-E' IN THE PASSAGE OF 'R+GS

ACROSS CELL MEMBRANE

1& Li%i 'i44)sion .Sim%#e 'i44)sion#

- drug molecules dissol*es in the mem(rane to &enetrate through the other side. Can take &lace either *ia

i&o&rotein mem(rane

Paracellular s&aces

,& A)eo)s 'i44)sion .Fi#tration thro)"h Pores/

- the size of the drug molecule is relati*e to the size of the &ores.

- water solu(le drugs with molecular weight less than 3 Daltons are a(le to cross

the cell mem(rane (% &assing through the &olar &ores. E./. Ethanol 6A#? =rea A#

0& S%eci4ic Carrier Meiate Trans%ort S!stem Acti(e Trans%ort

- &rocess (% which a su(stance is trans&orted against a concentration gradient.Drug molecules are mediated (% trans&ort KcarrierL that furnish energ% for the

trans&ortation of drug from lower concentration through higher concentrations.

E./. a' Q' Ca' 8e' amino acids' and glucose.

9 8eatures

3. +(ilit% to work against concentration gradient' osmotic' electrical' or

h%drostatic gradient. $&ecificit% R a(ilit% to concentrate a selected su(stance on one side of the cell

mem(rane.

9. Each s%stem re/uire an energ% source +TP#' to which it is directl% cou&led.

Faci#itate 'i44)sion

- a &assi*e &rocess where(% drugs can mo*e across cell mem(ranes more ra&idl%than sim&le diffusion.

- in*ol*es the action of a s&ecific (ut satura(le carrier s%stem

- can onl% work in the &resence of an a&&ro&riate concentration gradient.

'ISTRIB+TION

- the &assage of drug into *arious (od% fluids com&artments such as &lasma' intestinal fluids

and intracellular fluids? &rocess (% which the drug (ecomes a*aila(le to (od% fluids and (od% tissues.

8actors affecting Distri(ution3. Blood flow

. +ffinit% to the tissue

9. Protein (inding

8orms of Drug inside the Bod%

3. 8ree ! =n(ound state - free acti*e drug

55


45/95


DCB

. Bound - inacti*e drug

Binding to Plasma Proteins - e./. salic%lic acid and warfarin (ind to +l(umin

Basic drugs (ind to acid gl%co&roteins and li&o&roteins Binding to Cells - drugs (ecome (ound onto the surface or inside the cells.

2nl% free drugs or drugs not (ound to &rotein are acti*e and can cause a &harmacologic res&onse. +s the free drug in the tissues decreases' more (ound drug is

released from the &rotein to maintain the (alance of free drug.

Checking the &rotein-(inding &ercentage of all drugs administered is im&ortant in order to a*oid &ossi(le drug to)icit%. E./. Drug accumulation and to)icit% can result if

two highl% &rotein-(ound drugs are gi*en concurrentl% (ecause the% will com&ete for &rotein

(inding sites causing more free drug to (e released into the circulation? +lso' a low &rotein

le*el decreases the num(er of &rotein (inding sites' causing an increase in the amount of free drug in the &lasma. Drug o*erdose ma% result (ecause drug dosage is &rescri(ed

according to the &ercentage in which the drug (inds to &rotein.

$T2F+GE DEP2T on-s&ecific $ite# - hel&s &re*ent &rolong the action or areas for transient storage.

+8800TH T0$$=E$ - ma%(e sites of action or areas for transient storage? some drugs

accumulate in &articular tissues such as fat' (one' li*er' e%e' and muscle.

E.g. Guanethidine - (inds to heart and skeletal muscle

uinacrine - (inds to li*er and skeletal muscles

Tetrac%cline - (one and enamel

Thio&ental - adi&ose tissue

METABOLISM

- i*er R main organ of meta(olism - most drugs are inacti*ated (% li*er enz%mes and are then con*erted (% he&atic enz%mes to

an inacti*e meta(olite or water solu(le su(stance for e)cretion. ,owe*er' some drugs are

transformed into acti*e meta(olites causing an increased &harmacologic res&onse. E)am&le of li*er disease that affects meta(olism - cirrhosis and he&atitis.

3. E)cretion in the original form e./. ,e)amethonium R a highl% ionized antih%&ertensi*e

com&ound e)creted in the urine unchanged.. Transformation into one or more Meta(olites

2ther organs G.0.T.' ung' kidne%' skin and &lacenta.

B02TF+$82FM+T02 - a &rocess wherein &arent drug is con*erted (% enz%mes

into drug meta(olites read% to &erform its action.

Biotransformation of Drugs has Two Effects

3. 0t alters the &harmacological acti*it%' usuall% decreasing it (ut sometimes con*erting

the drug to a com&ound similar or greater acti*it% &otenc%# than the original.

. Fesults in meta(olites that are more water-solu(le and less li&id solu(le than the &arentcom&ounds and therefore more readil% e)creted in the urine.

56


46/95


DCB

Two General T%&es of Chemical Feaction

9hase 4;on-S)nthetic reaction

3. 2)idation - Diaze&am. Feduction - itraze&am' Cortisone

9. ,%drol%sis - $u)amethonium' +methocaine

9hase < 4S)nthetic 4=on2ugation Reaction

-0t in*ol*es con7ugation to form one or more of the following

3. Glucoronide e.g. Mor&hine' Paracetamol. $ul&hate e.g. 0so&renaline

9. +cetate e.g. 0soniazid' ,%dralazine

6. Glutathione e.g. Paracetamol

BIOLOGIC HALF3LIFE .t1=,/ - is the time it takes for one half of the drug concentration to

(e eliminated.

- a drug goes through se*eral half-li*es (efore more than 5I is eliminated.

E)am&le A


47/95


DCB

CHT2C,F2ME P6CRETION

- ma7or wa% (% which the acti*it% of the drug is terminated

- mainl% in the Qidne%? some *ia the E)tra Fenal Foute# .Bile' $kin sweat#' ungse)&ired air#' $ali*a' 8eces

and Breast Milk

- e)&ressed in terms of KFenal Plasma ClearanceL R the *olume of &lasma effecti*el% cleared of the drug (% the kidne% in unit time.

FE+ ECFET02 - most im&ortant route of drug elimination

9 Processes 0m&licated in Fenal E)cretion3. Glomerular 8iltration

- de&ends u&on the &lasma concentration of drugs and molecular weight.

- 3< ml.!min.

. "u,ular Rea,sorption > +cti*e $ecretion in the Pro)imal tu(ule 9. "u,ular Secretion ! Passi*e Fe-a(sor&tion in the distal tu(ule

PHARMACO'YNAMICS

Is the Drug producing the reuired 9harmacological &ffect# - stud% of a drugOs effect on cellular &h%siolog% and (iocehmistr% and the drugOs mechanism

of action.

0. Drugs which act *ia Pharmacological Fece&tors3. +ct at low concentration

. Feact with s&ecific rece&tors

9. $how structure acti*it% relation6. Can (e antagonized (% s&ecific antagonist

e./. acet%lcholine? adrenaline? noraduraline and histamine

e 00. Drugs which D2 2T act *ia Pharmacological Fece&tors

f 3. +ct at higher concentrations

g . Do not react with s&ecific rece&tors

h 9. Tend to show structure-acti*it% relationshi&si 6. Do not ha*e s&ecific antagonists

e./. General anesthetics and non-s&ecific destructants of cell mem(ranes such as

detergents.

'R+G3RECEPTOR INTERACTION

Rece%tor - a macromolecule with s&ecial sites to which s&ecific su(stances (inds.Drug!igands R Fece&tor#.

$0TE$ 28 FECEPT2F$

3. 2n or within Cell Mem(ranes. 0nside Cells

59


48/95


DCB

Most rece&tors' &rotein in structure' are found on cell mem(ranes. Drugs act through

rece&tors (% (inding to the rece&tor to &roduce initiate# a res&onse or (lock &re*ent# a

res&onse. The acti*it% of man% drug is determined (% the a(ilit% of the drug to (ind to a s&ecific rece&tor. The (etter the drug fits at the rece&tor site' the more (iologicall% acti*e

the drug is. 0t is similar to the fit of the right ke% in a lock.

Fi")re Two drug agonists attach to the rece&tor site. The drug agonist that has ane)act fit is a strong agonist and is more (iologicall% acti*e than the weak agonist.

A"onist - a drug hormone or neurotransmitter# which com(ines with its s&ecific rece&tor'

acti*ates it and initiates a se/uence of effects.

E./. 0so&roterenol stimulates the (eta3rece&tor.

Anta"onist - a drug which interferes with the action of an agonist (ut does not ha*e an%effect itself unless it &ossess &artial agonist acti*it%.

E./. Cimetidine (locks the ,rece&tor thus &re*enting e)cessi*e gastric

secretion.

Partia# A"onist - a drug that act on a rece&tor with an intrinsic acti*it% or efficac% of X 3.

Mi$e A"onist3Anta"onist - a drug that act simultaneousl% on a mi)ed grou& of rece&tor with an agonist action on one set and an antagonist action on another.

'R+G ANTAGONISM 3 occurs when their (iological effect is less than the e)&ected sum of

their indi*idual effects. P'armacological Antagonism)

3. Fe*ersi(le Com&etiti*e ! E/uili(rium +ntagonism

- su(stances are com&eting d%namicall% for the same &harmacological rece&tor. 0rre*ersi(le Com&etiti*e ! on-E/uili(rium +ntagonism

- drugs form *er% strong (onds

on+ometitive Antagonism - (lock action of an agonist not at the rece&tor le*el (ut atsome &oint (etween rece&tor and effector that leads to the action of the agonist.

P'(siological Antagonism - occurs when two drugs that act on different rece&tors &roduce

o&&osite effects. E./. +drenaline antagonizes the effects of histamine on (ronchial

smooth muscle.

+'emical Antagonism - occurs when one drug com(ines chemicall% with another to

&roduce inacti*e &roduct.

5;


49/95


DCB

P'armacoinetic +ntagonism - occurs when one drug effecti*el% reduces the

concentration of another at its site of action (% altering its a(sor&tion' distri(ution or

elimination.

Re#ationshi% Bet


50/95


51/95


DCB

THPE$ 28 ,0$T+M0E FECEPT2F$

H1 @ &rimaril% related to smooth m. acti*it%

H, @ &rimaril% in*ol*ed with the stimulation of gastric secretions

H0 @ mediates C$ effects of histamine on histaminergic ner*e terminals

E44ects o4 Histamine

,eart - increase heart rate Y force of contraction which results in an increase in cardiacout&ut

- increase histamine ma% cause arrh%tmias due to slowing of +- conduction

- dilation of small (.* leads to flushing' lowered &eri&heral resistance' and a dro& in (lood &ressure.

$mooth muscles - KBronchial muscleO - acti*ation of ,3rece&tor results to (ronchoconstriction.

- Patients who suffer from asthma are &articularl% sensiti*e to the action of histamine on

the (ronchial musculature howe*er' antihistamines are of no *alue in the treatment of asthma.

Gastric secretion - e*en a slow concentration can cause co&ious secretion of the gastric

7uices mediated (% , rece&tor. Pain and 0tch - caused (% direct stimulation of free ner*e endings when in7ected.

- $u(cutaneous in7ection of histamine causes shar& &ain of short duration like a was&Os

sting (ut when in7ected into a more su&erficial la%er of the skin' causes itching.

ANAPHYLA>IS AN' ALLERGY

Ana%h!#actic reactionR most dangerous acute allergic reaction occurring hour after drug

administration. - histamine will (e released due to an antigen com(ining with s&ecific anti(od% attached

to the surface of mast cells DEGF+=+T02# causing the e)trusion of histamine

from the secretor% granules in the mast cells. - e./. of su(stances that can cause ana&h%la)is and allerg% Penicillin' animal fur'

&ollen.

A(erse E44ects- undesira(le clinical action of a drug? a range of untoward effects

unintended and occurring at normal doses# of drugs that cause mild to

se*ere side effects' including ana&h%la)is? +lwa%s undesira(le.

Sie E44ects - are &h%siologic effect not related to desired rug effects? Ma%(e desira(le or

undesira(le and are &redicted.

To$ic E44ects - ad*erse effects of an une)&ected nature resulting from the direct actionof a drug.

A##er"! - altered ca&acit% of the (od% to react to *arious antigens.

Iios!ncracies- co*ers unusual or (izarre drug effects that cannot readil% (e e)&lained in an

indi*idual reci&ient.

A+TOCOI'SR deri*ed from the Greek word KautosL self# and ZakasL remed%#. 0t refers

61


52/95


DCB

su(stances which ha*e local hormone-like acti*it% at or near the site of

&roduction.

EICOSANOI'SR a term that denotes the meta,olitesof certain -car(on

&ol%unsaturated fatt% acids' mainl% arachidonic acid.

- &roducts of arachidonic acid meta(olism are di*ided into two main grou&s on the (asis that the% are ultimatel% deri*ed from the action of one of the two enz%mes

s%stems c%clo-o)%genase or li&o)%genase# on arachidonic acid.

+F+C,0D20C +C0D - a - &ol%unsaturated fatt% acid

Two sources

3. Meta(olic &ool - endogenous s%nthesis of arachidonic acid

. Cell mem(rane &ool - stimulated s%nthesis such as trauma? ma7or source of theeicosanoid &recursor in inflammation.

+rachidonic acid -----meta(olized------ results to meta(olites eicosanoids - a term[# (% the action of the enz%me c%clo-o)%genase and li&o)%genase#

0n most cells and tissues' &hos&oli&ids are thought to (e the ma7or source of arachidonic acid.

3. The first ste& in eicosanoid s%nthesis li(eration of the +rach. +cid from cell mem(rane &hos&oli&ids (% the action of a grou& of enz%mes known as the &hos&oli&ases &articularl%

&hos&oli&ase +res&onsi(le for its (ulk.

. The second ste& formation of c%clo-o)%genase on free arachidonic acid results in the

insertion of o)%gen molecules into the fatt% acid car(on chain to form PGGwhich is ra&idl% transformed (% the &ero)%dase-like acti*it% of c%clo-o)%genase into the

h%dro)%&ero)ide' PG,#. This is followed (% the formation of one of the three grou&s

de&ending on the &articular cell and circumstances in*ol*ed' the &rostaglandins' throm(o)ane' and &rostac%clin.

CYCLO3O>YGENASE PRO'+CTS

PROSTAGLAN'IN 33stidentified in 359 (ut their structure and function were

elucidated until 35A.

- occur in e*er% tissue and (od% fluid.

* *asodilators @ fall in (lood &ressure

< ")pes: PGE and PG8 series

THROMBO>ANEAN' PROSTACYCLIN "(R%?@%A;& A


53/95


DCB

LIPO>YGENASE PRO'+CTS

LE+DOTRIENES - has &otent chemotactic &ro&erties? &ro(a(l% in*ol*ed in the

&rocess of cellular infiltration that accom&anies

inflammation. T%&es T+6? TB6? TC6? TD6? TE6

PLATELET ACTI-ATING FACTOR

- a li&id autocoid s%nthesized mainl% (% &latelets' leukoc%tes' and endothelial cells. - action includes *asodilation' inc. in *ascular &ermea(ilit%' white (lood chemota)is'

and the release of l%sosomal enz%mes.

- a &otent stimulator of &latelet aggregation.

- ma% also (e im&ortant in the &athogenesis of asthma.

Arachionic Aci Meta?o#ism Pro)ct

C!c#o3o$!"enase %ro)ct Li%o$!"enase %ro)ct

Prosta"#anins Le)kotrienes

Throm?o$anes Com%o)ns ?ase on

Prostac!c#in eicosatetraenoic aci

BRA'YDININ AN' DALLI'IN

- Pol%&e&tides formed from the &lasma al&ha glo(ulins (% a com&le) series of

&roteol%tic reactions.

- Potent *asodilators - 0ncrease ca&illar% &ermea(ilit% @ oedema

- Cause (ronchoconstriction

- Brad%kinin 3 acti*e than histamine? effects are (rought (% Binin Receptors B3

and B

63HY'RO>YTRYPTAMINE .63HT/

7 - amine formed (% the h%dro)%lation of tr%&to&hanstored in gastric mucosak - dilatation of arteries and constriction of *eins *ia rece&tors


54/95


DCB

+ctions of %m&hokines

3. Chemotactic for macro&hages. Macro&hage acti*ation

9. Macro&hage inhi(ition

6. Chemotactic for other mononuclear 1BC


55/95


DCB

63HT ANTAGONISTS- Ergot alkaloids are a grou& of com&ounds that are antagonists for


56/95


DCB

6. G+TE C2TF2 Theor% - stressed the im&ortance of (oth descending control

mechanism and acti*it% in large sensor% fi(er in modulating the &ain e)&erience.

PEF0P,EF+ MED0+T2F$ 28 P+0

3. BF+DHQ00

. ,0$T+M0E9. E0C2$+20D$

8our Main Grou&s of Eicosanoids3. Prostaglandin

. Prostac%clin

9. Throm(o)ane

6. eukotrienes

CETF+ MED0+T2F$ 28 P+0

3. +mino +cids. Pe&tides

MET,2D$ T2 FE0EE P+03. Femo*e &eri&heral stimulus

. 0nterru&t nocice&ti*e in&ut

9. $timulate nocice&ti*e inhi(itor% mechanism

6. Modulate central a&&reciation of &ain and!or emotional concomitants


57/95


DCB

6& Sa#ic!#amieR internal use as an analgesic? less effecti*e than as&irin? less G.0.

irritation.

7& 'i44#)nisa#R an in*estigational salic%late? &ossi(l% (etter tolerated ' effecti*e at lowerdoses? a&&arent thera&eutic ad*antage o*er as&irin and &erha&s other inflammator%

agents.

ASPIRIN

- a(sor(ed from the git? &artl% from stomach (ut mainl% in the u&&er small intestine

Pharmaco#o"ica# Pro%erties

3 +nalgesic mild analgesic# R due to inhi(ition of the s%nthesis of PGE.

$uita(le regimen A-3mg. e*er% 6-A hours.

- +nti-inflammator% R inhi(it s%nthesis of eicosanoids? ,igh concentrations can inhi(it the function and acti*it% of PM leukoc%tes

- +nti&%retic R lowers an ele*ated (od% tem&. &%re)ia# due to infection' tissue damage'

malignanc% or other disease states? due to inhi(ition of &rostaglandin

&roduction in the h%&othalamus. - +ntithrom(otic effect

+n


58/95


DCB

A. Do not affect uric acid e)cretion

:. Enhances water trans&ort in the kidne%.

4. Peak &lasma concentration usuall% occur 9 minutes. +fter dosage' and the half lifeis usuall% hours.

5. Con7ugated in the li*er and e)creted in the urine.

+d*erse Effect

3. Methemoglo(inemia Phenacetin#

- condition that results from con*ersion of the iron in hemoglo(in to an o)idized statethat cannot effecti*el% carr% o)%gen.

$igns 3. C%anosis

. D%s&nea on e)ertion

9. +nemia

. ,emol%tic +nemia

- ,emol%sis is caused (% minor meta(olites that o)idize glutathione in the FBC and

there(% la(ilize the er%throc%te mem(rane to o)idati*e destruction.$igns 3. +(dominal or lower (ack &ain

. ;aundice 9. ,emoglo(inuria

6. +nemia

9. ,e&atic ecrosis

- ma% occur after ingestion of a single dose of 3 to 3< Grams.

6. e&hroto)icit%+dult dose 9< to


59/95


DCB

. +nalgesic' anti&%retic' and anti-inflammator%.

9. 0ndicated for the s%m&tomatic treatment of rheumatoid arthritis.

+d*erse Feaction

3. Gastointestinal u&set

. C$ effects such as dizziness' headaches' drowsiness and tinnitus.

a&ro)en t3! 39 hours.

0(u&rofen R &eak &lasma concentration R 3.< hrs. after dosage and the &lasma half life is hours? (roken down in the li*er? e)creted in the urine? has similar

unwanted effects as as&irin.

B& IN'OLEACETIC ACI'

3. 0ndomethacin

- most &otent inhi(itors of c%clo)%genase

- analgesic' anti&%retic' &owerful anti-inflammator% agent.

- used in rheumatoid arthritis.- first drug of choice to treat gout.

+d*erse reaction- G0 com&laints

- C$ - dizziness' headache' tinnitus' *ertigo' confusion R unknown' (ut ma% (e

due to PG inhi(ition. $ulindac

- has analgesic' anti&%retic effect.

- treatment of rheumatoid arthritis.

C& PYRROLACETIC ACI'

Tolmentin

Jome&irac

'& FENAMIC ACI' 'ER-IATI-ES .FENAMATES/

3. Mefenamic acid- treatment of &ain' d%smenorrhea

- sedation can occur

- a(sor(ed after oral dose? &eak &lasma concentrations R after hrs.? half-life is 9-6

hours.- meta(olized in li*er' half of meta(olites e)creted in the urine' half in the feces.

- Diarrhea occurs in


60/95


DCB

F& 'IFFL+NISAL

- a difluoro&hen%l deri*ati*e of salic%lic acid? has similar &harmacologic &ro&erties asas&irin

- long &lasma half-life R 4 hrs. onl% (.i.d.#

II& NARCOTIC ANALGESIC $imilarities The% all &roduce

3. Potent analgesia. +ddiction

9. Fes&irator% de&ression

6. $edation


61/95


DCB

B& Coeine or Meth!# Mor%hine

- Dose +dult R 3


62/95


DCB

'& Ani#eriine

- Dose usual +dult dose R < to


63/95


DCB

Their a(use ma% lead to moderate or low &h%sical de&endence or high &s%chological

de&endence.

Drugs included was formerl% known as KClass B arcotic drugsL &lus a num(er of non-

narcotic agents. E./. Chlorhe)adol Gluthethimide

Meth%l&r%lon $ulfodieth%lmethane $ulfonmethane alor&hine Benz&hetamine Chlor&hentermine

Phendimetrazine

Certain (ar(iturates e)ce&t those listed in another schedule.

$C,ED=E 0 $=B$T+CE$

Drugs with low &otential for a(use that leads onl% to limited &h%sical or &s%chological

de&endence relati*e to drugs in $chedule 000.

E./. Bar(ital Pheno(ar(ital

Ethinamate Paraldeh%de

Phentermine Methohe)ital 8enfluramine Meth%l&heno(ar(ital

Chloral (etaine Chloral h%drate

Me&ro(amate Pro&o)%&hene Benzodiaze&ines Me(utamate

Ethchlor*%nol

$C,ED=E $=B$T+CE$

Drugs ha*e a lower &otential for a(use than those in $chedule 0 for which there is currentl%

acce&ted medical use in the =.$.

Drugs are categorized as KE)em&t arcotics.L

HEMOSTATICS ocall% a&&lied su(stances that are em&lo%ed to arrest e)cessi*e (leeding or hemorrhage.

S!m%athomimetics

- reduce (leeding (% local *asoconstriction. E./. E&ine&hrine

St!%tics an Astrin"ents

- &reci&itates the tissue &roteins in the immediate area.E./. Jinc Chloride' +luminum Chloride' 8erric $ulfate

Mechanica# A"ents

- acts as matrices in which (lood cells ! fi(rin can (e entra&&ed.E./. Gel foam' 2)idized Cellulose' 2)idized Fegenerated Cellulose.

Throm?in

- normal constituent of the (lood coagulation scheme' com(ines with fi(rinogen.

HEMOSTASIS AN' HEMOSTATIC AGENTS

70


64/95


DCB

8actors in the +rrest of ,emorrhage

1& -esse#


65/95


DCB

- decrease throm(in formation

E./. +s&irin' Di&r%damole' $ul&hin P%razone.

FIBRINOLYTIC 'R+GS

- &romotes the (reakdown of throm(i (% acti*ation of &lasminogen to form &lasmin.

E./. $tre&tokinase' =rokinase' Tissue Plasminogen +cti*ator.

ANTIFIBRINOLYTIC 'R+GS

- these encourage the sta(ilization of fi(rin (% inhi(iting &lasminogen acti*ator. E./. Trane)amic acid

- effects ausea' diarrhea' h%&otension.

'ENTAL MANAGEMENT OF PATIENTS ITH HEMOSTATIC PROBLEMS

1& Im%aire P#ate#et F)nction

- due to reduction in &latelet count or im&aired aggregation due to drug thera&%.

- Treatment ow &latelet count R Platelet transfusion (efore surger%. Throm(oc%to&enia due to immune destruction of &latelet R +dministration

of corticosteroid - it is a wise &recaution to suture and &ack the socket to minimize the risk of &ost

e)traction hemorrhage.

- drugs that im&air &latelet aggregation and increase (leeding time includes +s&irin' $+0DOs' $odium al&roate' and Phen%toin.

,& -asc)#ar 'e4ects

- associated with *itamin C deficienc% and long term corticosteroid thera&%. - &atients ha*e increased ca&illar% fragilit% which can cause (leeding &ro(lems after

surger%.

- can (e controlled (% &ressure' suturing' and &acking.

0& Im%aire Coa")#ation

A& Haemo%hi#ia

- se)-linked? affects onl% males. - &atients ha*e reduced factor 000 acti*it%.

- can (e corrected (% re&lacement thera&% of freeze-dried factor 000

cr%o&reci&itate#.

- drugs used in con7unction with factor 000 include anti-fi(rinol%tic agents' e&silonaminoca&roic acid which should (e started &re-o&erati*el%.

B& Christmas 'isease

- associated with a deficienc% of factor 0 deri*ed from &lasma (ut not &resent in

cr%o&reci&itate#.

- Fe&lacement thera&%.

C& -on i##e?rans isease

- inherited disorder associated with (oth &rolonged (leeding time and deficienc% of

factor 000. - re&lacement thera&% is necessar%.

76


66/95


DCB

LOCAL ANESTHETICS - re*ersi(le Blockade of Peri&heral er*e Conduction? drugs that ha*e little or no irritating effects when in7ected into the tissues and that will tem&oraril% interru&t conduction when

a(sor(ed into the ner*e.

A)tonomic Losses in the )s)a# orer

3. $ense of Cold

. 1armth9. Pain

6. Touch


67/95


68/95


DCB

DEPFE$$02 of certain areas of the (rain

Classic Progression 3. Festlessness' +&&rehension and Tremors &rogressing to E)citement and Con*ulsions

. 0ncrease Blood Pressure and Pulse Fate

9. 0ncrease Fes&irator% Fateo 6. Fes&irator% and cardio*ascular de&ression with oss of refle)es and consciousness.

Characteristics o4 Liocaine To$icit!

D&9R&SSI%; generall% the cause of Death' ma% a&&ear without initial stimulation.

GENERAL ANESTHESIA - the drug induced a(sence of the &erce&tion of all sensation allowing surger% or other &ainful

&rocedures to (e carried out.

- de&resses the C$? alle*iate &ain and cause a loss of consciousness.

,0$T2FH

itrous 2)ide Klaughing GasL descri(ed (% 7ohn Priest

,orace 1ells o(ser*ed its effects as anesthetics. Ether R (% T.G. Morton and C.T. ;ackson

,ighl% flamma(le' *olatile' &ungent odor.

Chloroform - *olatile li/uid? (% ;.H. $im&son

T,E2F0E$ 2 MEC,+0$M 28 +CT02 28 G.+.

3. i&id or Me%er 2*erton Theor%

. 0nhi(ition of (iochemical +ction9. Molecular theories

Pharmacologic Effects

3. C$ de&ressants. C$ de&ression

9. =rine out&ut is reduced

6. Ma% &roduce li*er damage.


69/95


DCB

,%&ertension

Tach%cardia

$tage 000 $=FG0C+ +E$T,E$0+

- state of analgesia associated with ma7orit% of surgical &rocedures

- s&ontaneous res&iration ceases

* E 9lanes ,ased on:

Fes&iration $ize of &u&ils

Refle' characteristics

E%e(all mo*ement

$tage 0 MED=+FH DEPFE$$02 ! FE$P0F+T2FH P+F+H$0$

- (egins with cessation of res&iration R circulator% colla&se

- Pu&ils fi)ed and dilated

- o lid or corneal refle)es 0f not re*erse immediatel%' Death occurs.

PHASES O% ANESTHESIA

8lagg#

IN'+CTION

- encom&asses all the &re&aration and medication necessar% for a &atient u& to the time the

surgeon is read% to (egin.

MAINTENANCE - (egins with the &atient at a de&th of anesthesia sufficient to allow surgical mani&ulationand continues until com&letion of &rocedure.

RECO-ERY

- (egins with the termination of the surgical &rocedure and continues through the &ost

o&erati*e &eriod until the &atient is full% res&onsi*e to the en*ironment.

CLASSIFICATION OF G&A& BY RO+TE OF A'MINISTRATION

In'alation Intravenous Agents

Gases -o#ati#e #i)is

itrous 2)ide ,alogenated ,%drocar(on eurole&tics

Chloroform 8entan%l with Dro&eridol

Eth%l Chloride 0nno*ar#C%clo&ro&ane Trichloroeth%lene

7:


70/95


71/95


DCB

=nwanted Effects ausea' omiting

AN>IOLYTICS - e./. Benzodiaze&ines- used orall% to &ro*ide &ost-o&erati*e sedation.

ANTIPSYCHOTICS eurole&tics# e./. Penothiazines deri*ati*es R &romethazine andTrime&razine.

- &re-anaesthetic sedati*es? anti-emetic? for &atients who fear or has &redis&osition to

&ost-o&erati*e *omiting? de&resses res&iration cause *ar%ing amount of h%&otension.

ANTICHOLINERGIC +tro&ine $ul&hate? ,%oscine? Gl%co&%rrolate

- reduce secretions? &re*ent o*eracti*it% of the &aras%m&athetic ner*ous s%stem.

Atro%ine S)#%hate- commonl% used to reduce sali*ar% and (ronchial secretions

during anesthesia (% antagonizing the actions of acet%lcholine at muscarinic

rece&tors.

H!oscine - antagonizes the effect of endogenous acet%lcholine at muscarinic rece&tors?

gi*en 0M 9-A minutes (efore induction anesthesia? a C$ de&ressant R causesdrowsiness and de&ression of the *omiting center -anti-emetic. +thigh doses' it ma%

act as stimulant of the C$. Both atro&ine and h%oscine (lock the action of

acet%lcholine released from the *agal ner*e endings which gi*es some &rotection

against *agal stimulation.

G#!co%!rro#ate - a /uarternar% ammonium? &roduces &rolonged and good control of

sali*ar% and &har%ngeal secretions? less effect on the cardio*ascular s%stem? used as &reo&erati*e or intrao&erati*e antimuscarinic

to attenuate or &re*ent the

intra-o&erati*e (rad%cardia sometimes associated with the use of su)amethonium or

due to cardiac *agal refle)es..

NE+ROM+SC+LAR BLOCDING AGENTS

- (% s&ecific (lockage of the neuromuscular 7unction' the% ena(le light le*els of anesthesia

to (e used with ade/uate rela)ation of the muscles of the a(domen and dia&hragm?&roduce rela)ation of the a(dominal muscles' and &aral%sis of the res&irator% muscles?

rela)es the *ocal cordsallowing the &assage of a tracheal tu(e.

T


72/95


DCB

and so does not significantl% alter the (lood &ressure. ,owe*er' if ra&idl% in7ected

0' it ma% cause a rise in (& due to *agal (locking and tach%cardia? does not cause

histamine to (e released? ma% also (e used to &roduce rela)ation in a num(er of &athological conditions such as tetanus? also used e)tensi*el% in 0C=.

Atrac)ri)mand -ecoroni)m - most often used at the &resent time? ha*e little effect

on the cardio*ascular s%stem? ma% release little of histamine? more ad*antageous to &atientOs with renal or he&atic im&airment.

00. DEP2+F0J0G M=$CE FE++T$

S)$amethoni)m - de&olarizes the &osts%na&tic mem(reane and maintains this state so

that the ad7acent m. fi(ers are electricall% ine)cita(le? in7ected 0? &roduces

com&lete muscular rela)ation in half a minute? has a num(er of muscarinic action including increase in sali*ar% secretion' muscle in7ur% occasionall% due to direct action on the muscle or ma% follow Q de&letion from muscles.? ma% cause

malignant h%&er&%re)ia R ma%(e treated (% ra&id cooling' inhalation of 3I

o)%gen and 0 of Dantrolene 3 mg!kg of (od% weight.

* ?S=+& =%;"RA="I%;

action &otential ---- tra*els down the motor ner*e---- release of &ackets of acth /uanta-millions of acth molecules# ----- acth crosses the s%na&tic cleft and interacts with the

cholinergic rece&tors on the end &late of a muscle fi(er ---- surge of acth (rings a massi*e

increase in the &ermea(ilit% of the &ost-s%na&tic mem(rane to a ions and to a X e)tent toQ ions a ions enter and generate a local end &late &otential de&olarization# until it

reaches a critical threshold --- triggers off a muscle action &otential &ro&agated along the

muscle fi(er causing it to contract.

+cth is then (roken down (% cholinesterase in the neuromuscular 7unction? the motor end&late &olarizes and is then read% to (e stimulated again.

IN'+CTION AGENTS .I- ANESTHETIC AGENTS/

- widel% used to induce anaesthesia

Soi)m Thio%entone - an ultra short acting (ar(iturate? gi*en 0? &roduces loss of consciousness in 3- seconds. Ma). de&th occurs 6 secs. ? &) (ecomes conscious -9

mins. after dosage? &ro*ide anes. for short o&erati*e &rocedures? induce unconsciousness

&rior to inhalation anaesthesia? ra&idl% enters the (rain? 4


73/95


DCB

Etomiate - a car(o)%lated imidazole deri*ati*e? ra&id reco*er% and lack of Khango*erO

effect ma% (e due to short &lasma half life? does not release histamine? &ainful' cause

in*oluntar% mo*ements? &rolonged use ma% cause adrenocortical su&&ression in 0C=?has little or no effect on the cardio*ascular s%stem.

Detamine - gi*en 0 (ut can (e gi*en 0M? associated with &rofound sedation and analgesia? &roduces dissociation (ut not sedation and so airwa% refle)es are maintained?

*i*id hallucinations and nightmares? raises (.&. and &ulse rate? useful in management of

mass casualties.

Pro%o4o# - a new &henolic 0 induction agent and maintenance anaesthesia &ro*ided the

surgical &rocedure does not e)ceed 3 hour.? reco*er% is usu. ra&id and often accom&anied

(% eu&horia? se)ual fantasies can also occur? highl% li&o&hilic? More e)&ensi*e. =nwanted effects - cardiac res&irator% de&ression? a&nea and marked h%&otensi*e effect?

&ain on in7ection.

INHALATION ANAESTHESIA

- most widel% used form of maintenance anaesthesia

0,++T02 ++E$T,ET0C +GET$

Nitro)s O$ie 3 E&& Entono$ colorless' odorless gas? weak anaesthetic? an ad7unct to

other inhalation agents? ma% &roduce se*ere h%&o)ia when used alone? an e)cellent

analgesic agent? a direct m%ocardial de&ressant? stimulates s%m&athetic ner*ous s%stem? ma% cause nausea' *omiting' megalo(lastic anemia and neuro&ath% in

animals#? su&&resses s&ermatogenesis and &roduction of 1BC and FBC in (one

marrow? =ses changing &ainful dressing' an aid to &ost-o&erati*e &h%siothera&% and emergenc% am(ulances.

Ha#othane - a halogenated h%drocar(on? colorless at room tem&erature? has &leasant

smell?not inflamma(le? non e)&losi*e? causes dose-related reduction in (.&.'slowing of heart rate? se*ere d%srh%thmia? (ronchodilation ? de&resses res&iration? no analgesic

&ro&ert% and does not &roduce a degree of rela)ation? ma% cause he&atic necrosis.

En4#)rane - a halogenated ether? colorless at room tem&erature? non flamma(le with a

mild sweet odor? alters electrical acti*it% in the (rain? 4I e)creted unchanged ine)&ired gases' .< I meta(olized in the li*er and e)creted in the kidne%? &roduces a

dose-related reduction in (.&.? causes res&irator% de&ression? twitching of the lim(s'

7aws' face and neck (ut self limiting? no significant effect on the li*er

Iso4#)rane - isomer of enflurane? a halogenated meth%leth%l ether? &h%sical &ro&erties

similar to enflurane? reduction in (.&. (ut has little or no effect on cardiac out&ut?

increase in heart rate (ut no arr%thmias? de&resses res&iration and stimulates airwa%

refle)es causing increased secretion' coughing and lar%ngos&asm. Ether - one of the earliest and safest *olatile li/uids irritating to the mucus mem(rane?

inflamma(le and e)&losi*e? often associated with nausea and *omiting? now rarel% used.

ANAESTHETIC EMERGENCIES

3. Fes&irator% 2(struction. ,%&ersensiti*it% reaction

90


74/95


DCB

ANTISEPTICS AN' 'ISINFECTANTS - su(stance that kill or &re*ent the growth of microorganism Antise%tics- used on li*ing tissues.

'isin4ectantsR a&&lied on inanimate o(7ects.

1& ALCOHOLS

A& Eth!# A#coho#and 0so&ro&%l +lcohol

B& Ch#orhe$iineand Ioine

C& S)r"ica# S%iritsR mi)ture of eth%l!meth%l alcohol

,& AL'EHY'ES

A&Forma#eh!eR (actericidal acti*it% on (acteria' fungi' and *iruses? action is *er% slow

R .


75/95


DCB

:. O>I'IKING AGENTSR li(erates o)%gen which o)idizes &roteins of (acteria and tissue

&roteins.

H!ro"en Pero$ieR mild antise&tic? 9I a/ueous solution to (leach discolored root

filled teeth? mouthwash in acute ulcerati*e gingi*itis.

Soi)m Per?orateR treatment of acute ulcerati*e gingi*itis? li(erates o)%gen when in

contact with organic matter.

1@&PHENOLS CREOSOLSand their deri*ati*es

Pheno#- 4I in water? irritant and caustic &roducing a (urning &ain? &roduces feeling of

anesthesia CMCPCam&horated &ara-amino&henol# R 9


76/95


DCB

Antimicro?ia# A"entsR su(stances that kill or su&&ress the growth or multi&lication or &re*ent

the action of microorganisms

Anti3in4ecti(e A"entsR su(stances that act against or tend to destro% infection.

Anti?acteria# A"entsR su(stances that destro% or su&&ress the growth or multi&lication of

(acteria.Anti(ira# A"entsR su(stances that destro% or su&&ress the growth or multi&lication of *iruses.

Anti34)n"a# A"entsR su(stances that destro% or su&&ress the growth or multi&lication of fungi.

Anti?iotic A"entsR chemical su(stances &roduced (% microorganisms that ha*e the ca&acit%' in dilute solutions' to destro% or su&&ress the growth or multi&lication of

organisms or &re*ent their action.

+nti(acterial +ntimicro(ials# R are o(tained from natural sources or are manufactured+nti(iotic R chemicals that are &roduced (% one kind of microorganism that inhi(it or kill another

kind of organism.

The difference (etween anti(iotic and s%nthetic anti(acterial agents is that anti(iotics are &roduced (% microorganisms and the anti(acterial agents are made in the la(orator%.

C#assi4ication o4 Anti?acteria#s Accorin" to its ACTION

3. BacteriostaticR inhi(it or retard the multi&lication or growth of (acteria (ut does not kill them.

E./. Tetrac%clines' sulfonamides' chloram&henicol

- (acteria can grow again when drug is withdrawn.

- ,ost defense mechanism e./. &hagoc%tosis# are re/uired to kill the microorganism.. Bactericia#R drugs that kill (acteria.

E./. Penicillin' Ce&halos&horins' +minogl%cosides' ancom%cin' Metronidazole'

0mi&enem. - (est choice in treatment es&eciall% in life threatening infections' endocarditis and in

&atients whose leukoc%te count is X


77/95


DCB

INFECTIONR in*asion of the (od% (% &athogenic microorganism and the reaction of the

tissues to their &resence and to the to)ins generated (% them.

Princi%a# 4actors that etermine a microor"anism ca)sin" an in4ection

3. irulence of the microorganism. um(er of organisms &resent

9. Fesistance of the host

Ho< o Microor"anism ca)se an in4ectionQ

3. 0nfecti*it% must enter the right &ortal of entr%#

. 0t must (e a(le to multi&l% on the (od% of the susce&ti(le host.

9. 0n*asi*eness effecti*e mechanism for transmission#6. 0t must (e a(le to &roduce to)ins' enz%mes and other meta(olites that affect the cell

or to)igenecit%.

Two Goals to (e achie*ed to &re*ent infection3. Feduce the num(er of (acteria in the surgical wound.

. Enhance the hostOs defenses so as to &re*ent the (acteria that entered the wound fromcausing clinicall% e*ident infection.

IN'ICATION FOR ANTIMICROBIAL AGENTS

A& Pro%h!#actic Inications- used for high risk &atients whose immune s%stem are weak. E./. in rheumatic or

congenital heart disease' Fenal dial%sis &atients' or the &resence

of a heart &rosthesis. +n% dental &rocedure ma% &reci&itate a (acteremia' therefore'

&ro&h%lactic anti(iotics must (e gi*en to &re*ent (acterial endocarditis.

B& Thera%e)tic Inication

- for the treatment of infection.

KDoes this &articular &atient need the assistance of antimicro(ial agents to resol*e this &articular infection>"

2T + 08ECT02$ FE=0FE +T0B02T0C T,EF+PH' it all de&ends on. "he patient. Khost res&onsesL

- Defense mechanism is considered.

- The &resence or a(sence of s%stemic manifestation such as fe*er' malaise' and

l%m&hadeno&ath% are indicators of how well the &atient is doing without antimicro(ial thera&%.


78/95


DCB

---------------------------------------------------------------------------------------------------------

+nti(iotics G- Y G G-

-------------------------------------------------------------------------------------------------------- Pheno)%meth%l Penicillin

Penicillin G

+m&icillin Er%throm%cin

Clindam%cin

Ce&halos&

Documents

Notes in Pharmacology - From Net