Ph.chem2 - Assign

7/28/2019 Ph.chem2 - Assign.

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PHARMACEUTICAL CHEMISTRY

PARTNER:

SUNSHINE A. BACLAAN

FATIMA JAY PARADERO

TOPIC:

PROTEINS, ENZYMES & PEPTIDE HORMONES

PROTEINS

Gelatin- Metabolism: Hydrolysis of Collagen- Occurs in sheets, shreds, flakes or coarse

powder. White or yellowish, has slight

characteristic odor & taste. Stable in dry air.

- Used in the preparation of capsules, coatingof tablets and with glycerin, as a vehicle for

suppositories.

- Used as a vehicle when slow absorption isdesired for drugs

- Used to replace loss in blood volume incases of shock

- Administered: IV (to increase clotting ofblood) or locally (to treat wounds in

hemorrhagic conditions).

Gelatin Film- Sterile, non-antigenic, absorbable, water

insoluble gelatin film

- Available as light yellow transparent brittlesheets (0.076 0.0228 mm thick)

Gelatin sponge [Gelfoam, Surgifoam]- Sterile, absorbable, water insoluble gelatin-

based sponge- Stable to dry heat at 150 for 4 hours- Absorb in 4-6 weeks when used as surgical

sponge

- Admin: topically (control capillarybleeding)

Venoms Cobra venom solution

- Injected IM as a non-narcotic analgesic indoses of 1 mL per day

Snake venom solution- Used subcutaneously in doses of 0.4 1 mL

as a hemostatic in recurrent epistaxis and

thrombocytopenic purpura & as a

prophylactic before tooth extraction &

minor surgical procedures

Stypven- From Russell Viper- Topically as hemostatic & thromboplastic

agent

Vein-apis- From Bees

- Topically in acute & chronic arthritis,myostitis & neuritis

Caerulein- From Frog/ red-eyed tree frog, Agalychnis

callidryas

- Used in radiography procedures to contractthe gall bladder

Sanvagine-

From Agalychnis callidryas- Used as anxiolytic

Bombesin- From European bellied frog- Used as anxiolytic

ENZYMES (proteins that have catalytic property)

Pancreatin [Panteric]- Cream-colored amorphous powder with a

faint characteristic odor.

- Dissolved slowly but incompletely in water;insoluble in alcohol

- Used largely for pre-digestion of food & forthe preparation of hydrolysates- Are digested by pepsin and acid in the

stomach

- Adult Dose: 325mg to 1gTrypsin Crystallized

- Proteolytic enzyme- Solubility in water and saline = 500, 000

units per 10mL

Pancrelipase [Cotazym]- Digestive aid- Used to help control steatorrhea and in

other conditions in which pancreaticinsufficiency impairs the digestion of fats in

the diet.

Chymotrypsin [Chymar]- Proteolytic enzyme- Used in cataract surgery

Dormase Alpha [Pulmozyme]- Used in cystic fibrosis because of its ability

to liquefy secretions from the lung

effectively

Hyaluronidase for injection [Alidase, Wydase]- Prepared from mammalian testes- Used to increase the spread and consequent

absorption of hypodermoclytic solutions; to

diffuse local anesthetics; and increase

diffusion & absorption of other injected

materials.

- Enhances local anesthesia in eye surgery- Practically nontoxic but may cause a local

infection to spread

- Should never be injected in an infected area- Sensitivity to the drug is rare

Imiglucerase Injection [Cerezyme]


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- Used to treat type 1 Gaucher disease Sutilains [Travase]

- Proteolytic enzyme- Used to dissolve necrotic tissue occurring in

2nd & 3rd degree burns as well as bed sores

& ulcerated wounds

- Contraindications: detergents & anti-infectives

- The antibiotic penicillin, streptomycin, &neomycin do not inactivate sutilains

Streptokinase [Kabikinase, Streptase]- Activates plasminogen to plasmin- Allergic reactions occur because of antibody

formation in individuals treated with it.

- Antibodies inactivate streptokinase &reduce its ability to prolong thrombin time

- Indicated for acute myocardial infaction(IV), for local perfusion of an occluded

vessel (Intra-arterial), and before

angiography (Intracoronary)

Urokinase [Abbokinase]- Plasminogen the only known substrate of

urokinase

- A direct activator of plasminogen- A non-antigenic and maybe used when

streptokinase use is impossible because of

antibody formation

- Administered: IV or Intracoronary routes Alteplase [Activase]

- A tissue plasminogen activator- Indicated for the IV management of acute

myocardial infarction.

Papain [Papase]- A light-brownish gray to weekly reddish-

brown granules

- Incompletely soluble in water- Best at a pH between 4 and 7- Used locally in conditions similar to those

for which pepsin is used

- Has been reported to cause allergies inpersons who are exposed to it

Bromelains [Ananase]- Used in the treatment of soft-tissue

inflammation and edema associated with

traumatic injury, localized inflammationand post-operative tissue reactions

- Available in 50,000 units tablets orally Diastase [Taka-Diastase]

- Yellow, hygroscopic, almost tastelesspowder

- Freely soluble in water- Used in doses of 0.3 1g in the same

condition as malt diastase

- Combined with alkalies as an antacid

HORMONES

PITUITARY HORMONES

Corticotropin Injection [ACTH inj., Acthar]- Exerts a tropic influence at adrenal cortex- pH range = 3 7- used for tis adrenocorticotropic activity

Respiratory Corticotropin Injection- Used intramuscularly for a more uniform

and prolonged maintenance of activity

Sterile corticotrophin Zinc HydroxideSuspension

- Dose: 40 units (IM) followed by amaintenance dose of 20 untis 2 or 3 times a

week

Cosyntropin [Cortrosyn]- Used as diagnostic agent to test for adrenal

cortical deficiency

- Dose: (IM or IV) Adult = 250 mg

Children (2 yrs below) = 0.125 mgGROWTH HORMONE

Somatrem (Systemic) [Protropin]- Administered: IM or SC- Therapy is continued as long as the patient

responds or until the patient reaches

mature adult height or until the epiphyses

closes

- Dose range: 0.05 to 0.1 IU Somatropin (rDNA origin) [Humatrope]

- Administered: IM or SC- Dose range: 0.05 to 0.1 IU

NEUROHYPOPHYSEAL HORMONES

Oxytocin Injection- Prepared by synthesis- pH = 2.5 to 4.5- expiration date = 3 years- widely used with or without amniotomy to

induce and stimulate labor

- administered: Injection or Sublingual Vasopressin Injection [Pitressin]

- Each mL possesses a pressor activity equalto 20 posterior pituitary units

- Expiration date = 3 years Vasopressin Tannate [Pitressin Tannate]

- Administered: IM (1.5 to 5.0 pressor unitsdaily)

- Useful for patients who have diabetesinsipidus

- Should never be used intravenously (IV) Felypressin

- Relatively low anti-diuretic activity andlittle oxytocic activity


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- Causes increase renal blood flow in the cat- 5 times more effective as a vasopressin

blood flow, especially in obstetrics and

gynecology

Lypressin [Diapid]- Available as topical solution, sprays, 50

pressor units (185 micrograms / mL) in 5-

mL containers

- Dosage (topical, intranasal): one or moresprays applied to one or both nostrils one

or more times a day

Desmopressin Acetate [Stimate]- Drug of choice: treatment of Central

Diabetes Insipidus because of its efficacy,

ease of administration (intranasal), long

duration of action, and lack of side effects

- Can be administered IM or IV also- Indicted in the management of temporary

polydipsia & polyuria associated with

trauma to, or surgery in, the pituitary

regionPANCRATIC HORMONES

Glucagon- Factor in the pathology of human diabetes- Regulation of the liver mediated

mobilization of stored glucose

- Principal consequence of highconcentrations of glucagon: Persistent

Hyperglycemia

- Exert hyperglycemic action; it affects theliver cells

- Inhibits the incorporation of amino acidsinto liver proteins- Fatty acid synthesis is decreased by

glucagon; cholesterol formation is also

reduced

- Activates liver lipases & stimulatesketogenesis

- Recommended for the treatment of severehypoglycemic reaction caused by

administration of insulin to diabetic or

psychiatric patients

- ADR: Nausea & Vomiting- Usual Dose:

Adult (paranteral) = 500microgram to 1mg repeated in 20

minutes if necessary

Pediatric = 25 microgram per kg ofbody weight repeated in 20

minutes, if necessary

GASTROINTESTINAL HORMONES

Pentagastrin [Peptavlon]- Functional group: AMIDE

- Indicated as diagnostic agent to elevategastric acid secretory function & is useful in

testing for anacidity in patients with

suspected pernicious anemia, atrophic

gastritis, or gastric carcinoma,

hypersecretion on suspected duodenal

output

- Administered: SC- Optimal Dose: 6 microgram / kg- Onset of action: 10 minutes after admin.- Peak response: 20-30 minutes- Duration of action: 60 80 minutes- Half-life (plasma): (


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Imiglucerase [Cerezyme]- Deficiency of imiglucerase causes gaucher

disease

- Indicated for the long-term replacementtherapy of Gaucher disease

- Admin: IV- Initial dose: 2.5 to 60 units/kg- Infused over 1-2 hours- The dose is usually repeated every 2 weeks- ADR: dizziness, headache, abdominal

discomfort, nausea, rash

Interferons- Exhibit antiviral & antiproliferative activity,

enhance phagocytic activity & augment

specific cytotoxicity of lymphocyte for

certain cells

- ADR: flu-like symptoms, bone marrowsuppression, neurotioxic effects,

hypocalcemia, anorexia, & other GI

symptoms & weight loss

Interferon Alfa-2a Recombinant [Roferon]- Used in the treatment of hairy cell leukemia

& acquired immunodeficiency syndrome

(AIDS) related kaposic Sorzoma

- Absorbed well after IM or IV admin.- Half-life: 5- 7 hours (IM route)- Solution store in refrigeration 36 to 46

degrees Fahrenheit

Peginterferon Alfa-2a Recombinant- Treatment of hepatitis C

Interferon Alfa-2a Recombinant [Intron A]- Treatment of hairy cell leukemia,

condyloma accuminata (genital warts),AIDS-related Kaposi sarcoma, Hepatitis C

and Hepatitis B

- Administered: IM or SC- Half-life: 2-3 hours (IM or SC) and 8 hours

(IV)

Interferon Alfa-n3 (inj.) [Alferon N]- Indicated by intralesional injection for

treatment of genital warts

Interferon Beta-1a [Rebif, Avonex]- Slow progression of multiple sclerosis as

well as the rate of relapse of this disease

Interferon Beta-1b, Recombinant [Betaseron]- Administered: IV, IM, SC, Intrathecal,

Intralesional

- Prevention of exacerbations in patientssuffering from relapsing / remitting

multiple sclerosis

- Dose: 8 million units (SC) every other day- Treatment of malignant glioma & malignant

melanoma

Aldesleukin [Proleukin]

- Treatment of adult metastatic renalcarcinoma

- Administered: IV infusion,- Dose: 10, 000 to 50, 000 Units / kg every 8

hours per 12 days

- Metabolized in kidney- No active form found in urine- Side effects: fever, hypotension, pulmonary

congestion, & dyspnea, GI bleeding,

respiratory failure, & renal failure, seizures,

and death.

Erythropoietin- Produce primarily by the peritubular cells

in the cortex of the kidney and up to 15% is

produced in the liver

- Erythropoietin levels decrease in patineswith renal fialure

Epoetin Alfa [Epogen, Procrit]- Indicated to patients with chronic renal

failure & anemia associated with aids

-Admin: IV

Colony stimulating Fators (Natural glycoproteins

produced in lymphocytes and monocytes)

Filgrastim [Neupogen]- Decrease incidence of fibril neutropenea in

patients with nonmyeloid malignancies

- Used within 24 hours Sargamostim [Leukine]

- Is a lineage-nonspecific hematopoieticfactor because it promotes the proliferation

and maturation of granulocytes and

monocytes- Primary indication: myeloid engraftment

following autologous bone marrow

transplantation and hematopoietic stem cel

transplantation.

Antihemophili factor [Humate-P, hemophil M,Koate HP, Monoclate P]

- A glycoprotein found in human plasma anda necessary co factor in the blood-clotting

mechanism

Antihemophilic Factor (Recombinant)[Kogenate, Helixate]

- Indicted for the treatment of hemophilia A- Administered: IV route- Temporarily prevents bleeding episodes in

hemophiliacs and may be used to prevent

excessive bleeding during surgical

procedures in these patients.

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Ph.chem2 - Assign