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==ANS==
**Holinergicki lekovi**
Lekovi sa indirektnim dejstvom
Lekovi sa direktnim dejstvom
- Estri holina (acetil holin, metaholin, karbahol, betanehol)
- Pilokarpin - Muskarin
Ireverzibilne antiholinesteraze
Reverzibilne antiholinesteraze
- Edrofonijum- Neostigmin- Fizostigmin
- Organofosfatni insekticidi (paraokson, paration, malation, OMPA)
- Bojni otrovi ( soman, sarin, tabun, VX)
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**Antiholinergicki lekovi**
Prirodni alkaloidi
Sintetske i polusintetske zamene
- Atropin - Skopolamin
Midrijatici
Spazmolitici
Antiparkinsonici
- Homatropin - Eukatropin - Tropikamid - Ciklopentolat
- Skopolamin-butil bromid (buskopan) - Metil-atropin
- Homatropin-metil nitrat - Drotaverin (no-spa)
- Triheksifenidil - Etilbenzatropin - Biperidin
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**Adrenergicki lekovi**Kateholamini
Adrenergicki vazokonstriktori
Adrenergicki bronhodilatatori
Adrenergicki stimulatori CNSa
- Adrenalin - Noradrenalin - Dopamin
- Nafazolin - Ksilometazolin - Oksimetazolin
- Efedrin - Fenilefrin - Metoksamin - Metraminol
Rezorcinoli
Sintetski kateholamini
Saligenini
- Izoprenalin
- Orciprenalin - Terbutalin - Fenoterol
- Salbutamol - Salmeterol
- Amfetamin - Metamfetamin
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**Antiadrenergicki lekovi**
Alfa adrenergicki blokatori
Beta adrenergicki blokatori
Neselektivni
Selektivni (alfa1)
- Fenoksibenzamin - Fentolamin - Tolazolin
- Alkaloidi razane glavnice(ergotamin, ergometrin, ergotoxin)
(Metrilergometrin, metisergid, bromokriptin)
(dihidroergotamin, dihidroergotoxin)
- Prazosin - Terazosin - Doksazosin
Neselektivni
Selektivni
- Propranolol - Oksprenolol- Alprenolol
- Timolol - Karvedilol- Sotalol
- Atenolol - Esmolol- Metoprolol
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**Antihistaminici**
H1 - antihistaminici
H2 - antihistaminici
- Difenhidramin - Dimenhidrinat - Prometazin
- Loratidin
- Hlorpiramin - Hlorfenamin - Feniramin
- Oksatomid - Astemizol - Terfenadin
- Cimetidin - Ranitidin
- Famotidin - Nizatidin
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==CNS==**Anksiolitici**
Benzodiazepini
Ostali anksiolitici
- Diazepam - Bromazepam - Lorazepam - Midazolam
- Buspiron - Zolpidem - Mepbromat
**Antidepresivi**Triciklicni Antidepresivi
- Amitriptilin - Protriptilin - Imipramin - Hlorimipramin - Doksepin
Inhibitori MAO- Nialamid - Tranilcipromid - Pargilin
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Selektivni inhibitori preuzimanja serotonina
Ostali
- Fluoksetin - Fluvoksamin - Paroksetin - Sertralin
- Moklobemid - Mianserin - Maprotilin - Trazodon
**Neuroleptici (antipsihotici)**Fenotiazini
Grupa 1 (izrazeno neurolepticko dejstvo)
Grupa 2 (izrazeno ekstrapirimidalno dejstvo)
Grupa 3 (izrazeno antiholinergicko dejstvo)
- Hlorpromazin - Levopromazin- Promazin
- Perfenazin- Flufenazin
- Tioridazinwww.belimantil.info
Butirofenoni
Ostali neuroleptici
Tioksanteni- Klopentiksol -Flupentiksol- Hlorprotiksen
- Droperidol- Haloperidol
- Litijum
- Klozapin
Stabilizatori raspolozenja
**Psihostimulansi**Kortikalni Medularni
-Metilksantini
( Kofein, Teofilin, Teobromin)
- Amfetamin - Inhibitori MAO
- Pentazol
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**Barbiturati**Intravenski anestetici
Lekovi protiv epilepsije
- Fenobarbiton-Na
- Tiopenton-Na
- Fenobarbiton
**Miorelaksansi**Depolarizujuci miorelaksansi
Nedepolarizujuci miorelaksansi
- Vekuronijum
- Sukcinil-holin
- Pankuronijum
- Galamin- Atrakurijum
- Rokuronijum
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**Anestetici**
Lokalni anestetici
Intravenski anestetici
Inhalacioni anestetici- Halotan - Enfluran - Izofluran - Metoksifluran
- Desfluran - Sevofluran - Azot-suboksid (azotni oksidul)
- Tiopenton-Na - Ketamin - Pentobarbiton-Na
- Propofol- Etomidat -Midazolam
Amidnog tipa
Estarskog tipa
- Lidokain - Mepivakain - Bupivakain
- Prokain - Tetrakain - Kokain - Benzokain
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**Opioidni analgetici**
Alkaloidi opijuma i polusintetske zamene
Sintetske zamene za morfin
- Morfin - Kodein - Heroin
- Meperidin - Metadon - Fentanil - Pentazocin - Tramadol
- NaloksonMorfinski antagonisti - Naltrekson
**Antipireticki analgetici**Derivati salicilne kiseline
Pirazoloni
- Acetil salicilna kiselina - Salicilamid- Na-salicilat
- Aminofenazon - Noraminofenazon-metamizol (analgin, novalgetol)
- Paracetamol
Derivati para-amino fenola- Fenacetin
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**NSAIL**Selektivni i specificni COX-2 inhibitori
Derivati propionske kiseline
Derivati sircetne kiseline
Derivati oksikama
Derivati pirazolona
Antireumatici drugog reda
- Meloksikam -Etodolak
- Ibuprofen -Naproksen -Flurbiprofen
- Piroksikam -Tenoksikam -Meloksikam
- Diklofenak -Etodolak -Indometacin
- Azapropazon -Fenilbutazon
- Hlorohin -Soli zlata -Imunosupresivi -TNF blokatori
- Celekoksib -Rofekoksib
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**Th Epilepsije**1) Fenitoin
2) Karbamazepin
4)Valproinska kiselina
3) Fenobarbiton
5) Oksazolidini (Primetadion i Parametadion)
6) Sukcinimidi (Etosukcimid)
8) Inhibitori ugljene anhidraze (Sultiam, Acetazolamid)
9) Vigabatrin
7) Benzodiazepini (Diazepam, Lorazepam, Klonazepam, Nitrazepam)
- Kortikotropin i Prednizon
Th kod decijih spazama :
- Klonazepam i Nitrazepam
- Diazepam IV (po 1 mg do 30)
Th epi statusa
- Lorazepam (sporo iv infuz)
- Fenobarbiton IV (100, 200,
400 do 800 mg )
- Opsta anestezija
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**Th Parkinsonizma**1) Levo-dopa
2) Antiholinergici (Triheksifenidil, Etilbenzatropin, Biperidin)
3) Bromokriptin
5) Amantadin
6) Selegilin
4) Pergolid
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CNS Pharmacology
GABA
Synthesis and inactivation Isoniazid GABA
Synthesis Inhibits glutamate decarboxylase originally used for TB
Vigabatrin GABA Degradation
Inhibits GABA transaminase (GABA succinate semialdehyde)
Sodium Valproate GABA Degradation
Inhibits succinate semialdehyde dehydrogenase (succinate semialdehyde succinate)
Tiagabine GABA Reuptake Inhibits the GABA Na cotransporter
GABAA receptor (pentameric heteromer, Cl channel inhibitory) GABA Endogenous agonist Muscimol Agonist Bicuculline Antagonist competitive Picrotoxin Antagonist ion channel block Benzodiazepines Allosteric modulator binds preferentially
between and 2 subunits Barbiturates Allosteric modulator Neurosteroids Allosteric modulator carbolines Allosteric modulator General anaesthetic Allosteric modulator
GABAB receptor (GPCR - gi open K channel,block VGCC, bicuculline insens ) GABA Endogenous agonist Baclofen Agonist anti spasmodic in spinal cord Gamma hydroxyl butyrate Agonist date rape Phaclofen Antagonist 2-hydroxysaclofen Antagonist
Anxiety and GABA Buspirone 5 HT 1A partial
agonist ? feedback inhibitory effect
blockers Somatic anxiety by removing peripheral effects
Tricyclics and SSRI
Antidepressants ? overlap between chronic anxiety and depression
Barbiturates Allosteric activators GABAA
At high [ ] can open channel in absence of GABA. Low TI, tolerance due to hepatic enzyme induction, profound depression and dependence. Largely replaced by BZD but still used as anticonvulsant. Increase channel open time.
Benzodiazepine Allosteric activators
Safer higher TI. Only potentiates the action of released GABA. Increases
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GABAA frequency of opening and increases affinity for GABA. BUT dependence, hypnotic, tolerance (due to subunit change) and synergistic with alcohol and anti histamine. Some have long lived metabolites e.g. nordiazepam t1/2 = 60hr. Hang over (effects: anxiolytic, anticonvulsant, hypnotic, muscle relaxant)
Diazepam chlordiazepoxide
Benzodiazepine Anxiolytic long t1/2 metabolised to nordiazepam = hang over.
Nitrazepam Benzodiazepine Hypnotic short t1/2 wears off before am. Zaleplan Acts at BZD site short t1/2. Shows selectivity for 1 unit
(shown to be involved with hypnotic effect) hence without anxiolytic effects. (thought to be due to 2unit)
Flumazenil Antagonist at the BZD binding site on GABAA receptor.
Neurosteroids Allosteric modulator
Includes progesterone metabolites and dehydroxycorticosterone. Enhance agonist binding and Cl flux by increasing frequency of opening. May be able to open channel in absence of agonist.
carboline carboxylate
carboline Allosteric modulator
Inverse agonist at BZD site. Decreases frequency of opening and affinity for GABA.
Glycine (Spinal cord inhibitory [renshaw cell] pentameric receptor) Strychnine Competitive antagonist of glycine receptor. NOT
active at glycine site on NMDA receptor.
Glutamate
Reuptake Dihydrokainate Inhibits neuronal Na dependent uptake SITS Inhibits glial Na dependent uptake.
Ionotropic receptors AMPA (GluR A,B,C,D pentamer. Flip-flop, Q/R RNA editing GluRB) AMPA Selective agonist
Kainate (GluR5-7 KA1-2 pentamer. RNA editing, rapid desensitisation Kainate Selective agonist
NMDA (NR1(alternative splice) + NR2A,B,C,D. sites: glycine (+), pH (low - ), ion channel (Mg), redox (SH ^freq), Zn (-), polyamine (+/-), steroid (+) N methyl D aspartate Selective agonist Dizolcipine Antagonist Ketamine Antagonist (channel block)
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Magnesium Antagonist (channel block) Phenylcyclidine Antagonist angel dust! Glycine Co-agonist Dichlorokynurenate Antagonist at glycine site
Anticonvulsants Phenobarbitone GABAA modulator
(barbiturate) Suppress focus, against all but absence. Sedation and tolerance (hepatic enzyme induction) charged not easy to cross BBB
Diazepam GABAA modulator (benzodiazepine)
Suppress spread (less on focus) status epilepticus. Sedation and tolerance (subunit change)
Clonazepam GABAA modulator (benzodiazepine)
Suppress spread (less on focus) status epilepticus and tonic/clonic.
Tiagabine GABAA Reuptake Inhibits GAT-1 Involved in Na dependent uptake. Adjunctive in partials
Vigabatrin GABA inactivation Inhibits GABA transaminase (GABA SSA) Adjunctive in partials
Valproate GABA inactivation Inhibits SSADH (SSA succinate) AND Na channels. Hence increasing GABA and decreasing Na (synergistic effects). All types INCLUDING absence (other anticonvulsants may be contraindicative of absence. Also no sedation so useful for children, because cant afford to sedate children continuously affect learning
Carbamazepine Use dependent Na blockers
Prevent spread. Partials and tonic/clonic
Phenytoin Use dependent Na blockers
Prevent spread. All except absence. Metabolism saturation so need to increment dose slowly and titrate plasma to monitor concentration
Lamotrigine Use dependent Na blockers
Prevent spread. Partials and tonic/clonic
Valproate Use dependent Na blockers
Prevent spread. All types including absence. Useful for children. see above
Ethosuximide T type calcium channel blockers
Absence first line treatment
Trimethadione T type calcium channel blockers
Absence first line treatment
Gabapentin Calcium channel blockers
Adjunct to partials. Sedation. Role in pain can overdose
Levetiracetam N type calcium channel blockers
Adjunct to partials. ? effect on AMPA/Kainate
Flebamate Glutamate receptors
NMDA glycine site.
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Levetiracetam Glutamate receptors
AMPA and Kainate receptors. Partials and tonic/clonic.
Absence seizures Valproate Block VG Na channel Ethosuxamide, trimethadione Block T type Ca channel Lamotrigine Block VG Na channel and neuronal
Ca channel Levetiracetam N type Ca channel Carbamazepine, tiagabine, vigabatrin Contraindicated and enhance
absence seizures.
Cerebrovascular accident ischaemic damage. (save the penumbra!!) Drugs used Statins, ACEi, Low dose aspirin, anti inflammatory Future NMDA-R block (dizolcipine side effects) newer tolerated ones
like DEXTROMETHORPHAN. Zn chelators, free radical scavengers, anti-inflammatory, adenosine agonists, combined AMPA/NMDA block, ?synergy between NMDA-R block and antiapoptotic drugs.
Alzheimers disease (B amyloid plaques and neurofibrillary tangles due to hyperphosphorylated tau. Role of secretins in misprocessin of APP) Putative drugs for B amyloid generation
B secretase inhibition (b secretase KO is not harmful) B amyloid vaccination (caused brain inflammation in trials) anti-inflammatory (ibuprofen reduces plaque in a mouse model) plaque solubilisation/inhibition of formation cholesterol lowering agents
Tacrine, dunazepil, rivastigmine
AChE inhibitors, in line with the cholinergic hypothesis But weak effect for 12-24 months maimum.
DOPAMINE
Synthesis and inactivation Carbidopa and benserazide DOPA decarboxylase inhibition (note
all L aromatic aa are substrates at this enzyme trypyophan and histidine.)
Clorgyline, Selegiline MAO A and B inhibitors selectively at low concentration
Reserpine Blocks synaptic vesicle uptake of DA Amphetamine Promotes emptying of vesicles
increasing [DA]I thus decreasing efficiency of uptake process.
Cocaine, nomifensine, benztropine, amphetamine
Block Na DA cotransporter, raising DA t1/2 in extracellular space.
Dopamine receptors. D1 = gs D2 = gi Dopamine D1A < D1B
D2A > D2B Agonist
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Quinpirole D2A > D2B Agonist Flupenthixol Non selective Antagonist Sulpiride Non selective D2 Antagonist (atypical) Clozapine C>A=B Antagonist (atypical) Haloperidol A=C>B Antagonist (typical) Spiperone A=C>B Antagonist (typical)
Parkinsons Disease L-DOPA With carbidopa (save for brain) and Domperidone
(antagonise CTZ DA receptors). After 5-10yrs side effects 80% dyskinesias, choreiform movements, 60% decreased efficacy of drug, rapid on/off, psychosis/hallucinations (^DA in mesolimbic system) Because therapeutic window decreases (supersensitivity and more neurones dying) L-DOPA holidays may help. Now aim is to delay L-DOPA use.
Benztropine Muscarinic cholinergic antagonist dry mouth, constipation, blurred vision. 1st line treatment. BUT will exacerbate alzheimers symptoms pro-dementia
Sellegeline MAO-B inhibitor no cheese reaction. Delays requirement for L-DOPA for 1 year and may supplement it to allow a reduced dose.
bromocriptine, lisuride, pergolide
Dopamine agonists. May be used as an adjunct to L-DOPA. Reduces off time but may have more serious side effects than L-DOPA.
Entacapone, tolcopone
COMT inhibitor.
Domperidone Block peripheral DA receptors in the ChemoTrigger Zone. Adenosine A2A antagonist
Reduce activity of indirect pathway, decrease ACh activity, decrease cortical striatal input. No rapid on-off, no dyskinesias, synergistic with L-DOPA allowing reduced dose and prolonging onset of side effects.
Future Antioxidants, glutamate antagonists, glial derived neurotrophic factor (? Neurones simply dormant not dead), transplants.
Schizophrenia Chlorpromazine Fluphenazine Haloperidol Flupenthixol
A>B=C Antagonist
TYPICALS
Typical. Little effect on symptoms. 90% improve (60% on placebo) BUT side effects motor disturbance (D2A) and tardive dyskinesia (involuntary face and trunk movements) Reduce aggression apathy plus loss of emotion. Sedation (H1 block) Postural hypotension (1 block). Breast development and lactation (loss of inhibition by TI DA) and side effects of mACh block dry mouth, constipation and blurred vision. Shows how dirty drugs are.
Clozapine Sulpiride
A
Olanzapine Pimozide
ATYPICALS work. [Clozapine may cause agranulocytosis in ~1% of pt, therefore continuous wbc monitoring must be conducted, making the drug expensive and thus use is limited.
Clozapine, olanzapine Risperidone
5-HT2C inverse agonist; D2 antagonist
The realisation that inverse agonism had an effect to increase firing of VTA and thus has been found to increase DA in PFC and hence decreasing negative symptoms. Note, typicals are only 5-HT antagonists so the increase in VTA firing is less.
Clozapine [Typical + idazoxan]
D2 antagonist and 2 block
Also shown that 2 block may have and effect. Shown to reduce negative symptoms. Shows how clozapine is dirty!
Serotonin
5-HT1A (gi Raphe presynaptic inhibition) Buspirone Agonist (anxiolytic) partial Pindolol Antagonist
5-HT1B (gi presynaptic inhibition) Methysergide Agonist Pindolol Antagonist
5-HT1C (gi alters blood vessel diameter of brain) Sumatriptan Agonist (migrane therapy) Spiperone Antagonist
5-HT2A B C (gq excitation) (c-thought to excite GABA interneurones - VTA) -methyl-5-HT Agonist Ketanserin Antagonist
5-HT3 (ion channel depolarisation) Biguanides Agonist Ondansetron Antagonist (+chemo antiemetic)
DEPRESSION Phenelzine tranylcypromine
MAOi Non selective, irreversible. Thus cheese effect. Also must be careful because MAO ~2-3 weeks to be resynthesised thus if give drugs requiring ^ MAO activity can lead to fatal hypertension.
Moclobemide MAOAi Selective. No cheese effect since B still active. Reversible so other drugs can be administered immediately.
Imipramine, amytriptiline
Tricyclics Inhibit NA and 5-HT uptake. Dirty, having effects at other receptors 1, 2, H1 (block sedation), mACh (block dry mouth)
Nomifensine NA SRI
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Citalopram fluoxetine
SSRI Highly specific, long t1/2 3 weeks to Css. Nausea side effect (^5-HT in gut) overdose non lethal, efficacy in ~60%.
Mianserin Not fully understood. No action on monoamine uptake. 2 block (? ^NA by blocking autoreceptors) H1 block (sedation) 5-HT2A 5-HT2C block.
Iprindole Evidence against monoamine theory no effect on MA. Unknown mechanism, no sedation and may not be very efficacious
FUTURE Substance P antagonist failed at phase III CRH antagonist - ? implicated in stress induced depression. In phase III
Manic phases of depression (15% suicide so must be controlled) Lithium Inhibits IMP phosphatase Valproate Inositol uptake inhibition. Anticonvulsant Carbamezepine Anticonvulsant Lamotrigine Anticonvulsant Anti pshychotics
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==KVS==**Inotropni lekovi**
Kardiotonicni glikozidi (digitalis)
Beta agonisti
- Digoksin - Digitoksin
- Dopamin - Dobutamin
**Diuretici**Pravi diuretici
Diuretici sa brzim i snaznim dejstvom
- Furosemid - Torasemid - Bumetanid - Piretanid - Etakrinska kiselina
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Osmotski diuretici
Diuretici koji stede kalijum
Inhibitori ugljene anhidraze
Ostali diuretici
Diuretici umerene jacine (tiazidi)
- Hlorotiazid - Hidrohlorotiazid - Politiazid
- Bendroflumetiazid - Ciklopentiazid
- Amilorid
- Antagonisti aldosterona (Spironolakton, Proreron)
- Triamteren
- Acetazolamid
- Amonijum hlorid - Preparati zive
- Indapamid
- Diazoksid
antihipertenzivi
- Manitol - Urea - Glicerol
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**Vazodilatatori**Organski nitrati i nitriti
Sintetske zamene za NTG
- Nitroglicerol (gliceril-tri-nitrat) - Izosorbid mononitrat
- Pentaeritril tetranitrat - Natrijum nitrit - Pentanol nitrit
- Dipiridamol - Molsidomin
- Izosorbid dinitrat
**Th hipertenzije**Diuretici- Tiazidi (najvise Hlorotiazid)
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Antiadrenergicki lekovi
Direktni vazodilatatori
ACE inhibitori
- Hidralazin - Dihidralazin - Diazoksid - Minoksidil
- Na-nitroprusid - Ca-antagonisti
- Kaptopril - Enalapril - Lizinopril - Ramipril
- Fosinopril - Kvinapril - Cilazapril
- Alfa metil dopa - Klonidin - Rezerpin - Beta blokatori
- Blokatori adrenergickog neurona (Gvanetidin, Betanidin, Gvanoksan)
- Gangliski blokatori - retko
- Alfa blokatori (dihidroergotamin/toxin, prazosin, labetalol)
****Antagonisti angiotenzinskih receptoraCentralni antihipertenzivi
- Losartan - Valsartan
- Klonidin- Metildopa - Moksonidin
Jos treba napomenuti : ****
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**Antiaritmici**Stabilizatori celiske membrane
Adrenergicki beta blokatori
Lekovi koji produzuju akcioni potencijal
Antagonisti kalcijuma
- Hinidin
- Prokain amid
- Dizopiramid
- Lidokain
- Fenitoin
- Meksiletin
- Tokainid
- Flekainid
- Enkainid
- Propafenon
- Lorkainid
- Propranolol - Esmolol
- Bretilijum - Sotalol - Amjodaron
- Verapamil - Diltiazem - Nifedipin
**Th hiperlipoproteinemije**- Nikotinska kiselina (niacin)
- Fibrati ( Gamfibrozil, Klofibrat, Fenofibrat, Bezafibrat, Ciprofibrat)
- Statini (Fulvastatin, Pravastatin, Atorvastatin, Simvastatin, Lovastatin)
- Holestiramin i Holestipol
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ANTIARITMICI
Lekovi male terapijske irine, i sami su aritmogeni i daju se samo u ozbiljnim aritmijama koje moguda ugroze ivot.Ritam srca zavisi od stanja jonskih kanala (Na, Ca, K), kao i funkcije autonomnog nervnog sistema.U SA i AV voru glavni depolariui kon je Ca+, repolariui je K+, a u His-Purkinjeovim vlaknimaNa+.Mehanizmi nastanka aritmija:
1. Poremeaj stvaranja ritma.2. Poremeaj sprovoenja ritma.
a. Odloena naknadna depolarizacijab. Reentry objasniu ti.c. Stvaranje nenormalne pacemakerske aktivnosti (ishemija + poveana adrenergika
aktivnost).d. Srani blok (zbog povrede sprovodnog sistema)
Aritmije koje se lee su one koje stvaraju hemodinamske probleme i one koje ugroavaju ivot. To su:1. Atrijalna tahikardija, flater i fibrilacija.2. Supraventrikularne (AV) tahikardije (reentry u visini AV vora).3. Ventrikularna tahikardija moe da pree u flater i fibrilaciju.
ANTIARITMICI
I klasa Blokatori Na+ kanala grupa lokalnih anestetika.Blokiraju voltano zavisne Na+ kanale u Purkinjeovim vlaknima i miokardu.
Ia podgrupa: HINIDIN i slini lekovi deluju i na atrijalne i na ventrikularne aritmije.Ib podgrupa: LIDOKAIN i sl. deluju na ventrikularne aritmijeIc podgrupa: FLEKAINID i sl. deluju na ventrikularne aritmije.
II klasa blokatori ESMOLOL, PROPRANOLOL
III klasa Blokatori K+ kanala SOTALOL, AMIODARON najbolji su.
IV klasa Antagonisti Ca+ DILTIAZEM I VERAPAMIL
V klasa Meovita grupa DIGITALIS, ADENOZIN, K+, Mg+.
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I KLASA
Ia GRUPA hinidin, prokainamid, dizopiramidMehanizam delovanja i farmakoloki efekti. Blokiraju Na+ kanale onda kada su oni otvoreni iliinaktivirani, ali ne i kada su potpuno repolarizovani, tj. zatvoreni blokiraju ih samo kada rade. Timese postie selektivnost samo na one delove tkiva gde se stvaraju aritmije, na ono tkivo koje jedelimino depolarizovano ishemino tkivo i ono koje ima kratku repolarizaciju, kao u tahikardiji. Nanormalno tkivo, tj. normalnu frekvencu srca ne ometaju.Smanjuju nagib depolarizacije i 4. faze akcionog potencijala to dovodi do irenja AP i poveanjarelativnog refrakatarnog perioda.Takoe, dovode do irenja QT intervala.Imaju i antimuskarinske efekte (dizopiramid).Neeljeni efekti. Male su terapijske irine, toksini su na:
1. Kardiovaskularni sistem negativno inotropno dejstvo.2. CNS tinitus, glavobolje.
Cinhonizam trovanje hinidinom.3. Veoma proiren i bifazan QRS kompleks Torsade des Pointes4. Sistemski prokainamid sistemski lupus.
Indikacije. Daju se i za atrijalne i za ventrikularne poremeaje ritma.Interakcije. Sa kardiotoninim glikozidima nikako davati. Hiperkaliemija potencira toksinost ovegrupe lekova.
Ib GRUPA lidokainDaje se samo intravenski i intrahospitalno.Mehanizam delovanja i farmakoloki efekti. Najselektivniji je za Na+ kanale (u otvorenom stanju) uisheminom tkivu od svih antiaritmika. Zbog toga se daje u infarktu, a ne deluje na zdravo tkivo.Najvie deluje na depolarizaciju, uglavnom ne menja irinu AP i QT intervala, kao i refraktarni period.Neeljeni efekti. Manje je toksian za srce od Ia, ali je toksian za CNS. Hiperkalijemija poveavatoksinost.Indikacije. 1) Infarkt miokarda ventrikularne aritmije.
2) Aritmije usled trovanja digitalisom.Spadaju jo i mexiletin, tokainid i fenitoin.
Ic GRUPA flekainid, enkainid, propafenonDeluju na iste faze AP kao i Ia, ali je najmanje selektivan za Na+ kanale pa su najvie aritmogeni.Najopasniji su jer mogu izazvati naprasnu sranu smrt, naroito posle infarkta miokarda.Propafenon je noviji, moe se davati i u trudnoi.Indikacije. Daju se samo onda kad se aritmije ne mogu izleiti drugim lekovima:
1) Ventrikularna tahikardija koja preti da pree u fibrilaciju.
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II KLASA blokatori propranolol, esmolol, metoprololMehanizam delovanja i farmakoloki efekti. Simpatika stimulacija poveava nadraljivost srca,sprovodljivost i ulazak Ca+ u eliju. U ishemiji uvek postoji poveana aktivnost simpatikusa i ulazakCa+ to moe da dovede do ventrikularnih aritmija.Primenom -blokatora sve to se spreava. Takoe, oni smanjuju stvaranje cAMP-a to smanjujeulazak Na+ i Ca+ u eliju i sledstvenu depolarizaciju.Na EKG-u produavaju PQ interval.Indikacije. Daju se i za pretkomorske i za komorske aritmije, naroito postinfarktno.
III KLASA blokatori K+ kanala sotalol, amiodaron, bretilijumMehanizam delovanja i farmakoloki efekti. Blokiraju K+ kanale i deluju na fazu repolarizacije,ime produuju srani akcioni potencijal. Takoe, blokiraju i simpatiki sistem (sotalol je i -blokatori ima izraeno negativno inotropno dejstvo), kao i Ca+ kanale.Bretilijum je blokator adrenergikog neurona jer prazni depoe kateholamina.Amiodaron, pored blokade K+ kanala, blokira i Na+ i Ca+ kanale i -receptore. Jedan je od najboljihantiaritmika, a skoro uopte nije proaritmogen, ali je izuzetno toksian na nivou drugih organa:
1. Disfunkcija tireoidne lezde;2. Stvara depozite u koi i ronjai;3. Dovodi do plune fibroze;
Indikacije. Daje se kod refraktarnih aritmija, ali ne dugo. Ako mora due, onda se ugraujepacemaker.
IV KLASA Ca+ blokatori verapamil, diltiazemMehanizam delovanja i farmakoloki efekti. Blokiraju L tip Ca+ kanala u srcu ime smanjujusprovodljivost kroz sprovodni sistem, pa i u AV voru, usled ega dovode do produenja PQ intervala.Indikacije. Za pretkomorske aritmije.Neeljeni efekti. Deluju negativno inotropno na srce i smanjuju minutni volumen.
V KLASA meovita grupa1. Adenozin daje se i.v. u hospitalnim uslovima, deluje veoma kratko (20-30sec). Deluje
na K+ kanale ime hiperpolarie sprovodni sistem. Daje se kod supraventrikularnetahikardije umesto verapamila.
2. Digitalis za atrijalne tahikardije.3. Kalijum za ektopinu aktivnost, ali u viku je tetan jer dovodi do reentry aritmija.4. Magnezijum slian kalijumu, a daje se zajedno sa K+ kod aritmija usled trovanja
digitalisom.
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==Respiratorni==**Terapija bronhijalne astme**
1. Adrenergicki Bronhodilatatori
-Salbutamol -Terbutalin -Salmeterol -Fetnoterol
2. Antiholinergici
-Ipratropijum-bromid
3. Metilksantini
-Teofilin -Aminofilin
4. Stabilizatori Mastocita
-Kromolin (natrijum-kromoglikat) -Ketotifen
5. Antagonisti Leukotrijena
-Zileuton -Montelukast -Zafirlukast
6. Glikokortikoidi
-Beklometazon -Budesonid -Flunisolid -Flutikason
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**Ekspektoransi**
1. Ekspektoransi koji povecavaju dubinu sonog sloja - mukokinetici
-Voda -Ekspektorantne soli (KJ, NaJ, Bromheksin)
-Ipekakuana -Saponinske droge
2. Ekspektoransi koji menjaju konzistenciju gelnog sloja - mukolitici
-Mukolitici koji kidaju disulfidne veze (Karboksi-cistein, Acetil-cistein)
-Proteoliticki enzimi (tripsin, himotripsin, DNaza, elastaza)
3. Ekspektoransi koji smanjuju adhezivnost gelnog sloja - surfaktanti
-prirodni -polusintetski -sintetski
4. Ekspektoransi koji poboljsavaju aktivnost cilija
-adrenergici (izoprenalin, adrenalin, terbutalin)
-u manjoj meri i prednizon, KJ, aminofilin
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**Antitusici**
1. Centralni antitusici
Opijati
-Kodein -Noskapin -Folkodin -Dekstrometorfan
Sintetski centralni antitusici
-Butamirat -Fedrilat -Klofedanol -Pipazetat -Glaucin
2. Periferni antitusici
-Pentoksiverin
-Prenoksidiazin
-Sluzava sredstva (beli zlez)
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**Th peptickog ulkusa**Antacidi neutralizatori stvorenog HCl
Mukoprotektivi
- Al(OH)3 , AlPO4
- NaHCO3
- MgO, Mg(OH)2, MgCO3- CaCO3
- Mg-trisilikat
- Sukralfat- Mg-trisilikat
- Karbenoksolon
- Preparati koloidnog bizmuta
- Mizoprostol
Lekovi koji uklanjaju druge faktore
ERADIKACIJA HELICOBACTER PYLORI
- Amoksicilin 500mg 3x1- Metronidazol 400mg 3x1- Omeprazol 20mg 2x1
==GIT==
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Inhibitori stvaranja HCl
H2 antihistaminici
Antiholinergici
Inhibitori sekrecije gastrina
Inhibitori protonske pumpe
- Ranitidin - Nizatidin- Famotidin
- Somatostatin - Oktreotid
- Atropin - Skopolamin-butil-bromid - Oksifenciklimin - Pirenzepin
- Omeprazol - Lansoprazol
- Rabeprazol- Pantoprazol
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**Antiemetici**
1) Antimuskarinski lekovi
2) H1 antihistaminici
3) Antidopaminski lekovi
4) Antagonisti serotoninskih receptora
5) Piridoksin
6) Kanabinoidi
- Atropin - Skopolamin - Benzatropin
- Difenhidramin - Prometazin - Ciklizin- Buklizin - Meklizin
- Fenotiazini
(hlorpromazin)
- Metoklopramid - Domperidon- Bromoprid - Butirofenoni
(Haloperidol,
Droperidol)
- Ondasetron - Tropisentron - Granisentron
- Vit B6
- TetraHidroKanabinol - Nabilon - Levonantradolwww.belimantil.info
**Emetici**
**Spazmolitici**
**Prokinetici**
- Apomorfin - Ipekakuana- Iritantne soli
(CuSO4, ZnSO4,
Zn-Acetat)
- Drotaverin - Skopolamin-butil-bromid- Mebeverin
- Metoklopramid - Domperidon - Cisaprid
**Antidijaroici**-Opijati (ranije tinctura opii,
sad vise ne)
- Loperamid- Difenokslat
- Bizmut-silikat -Bioloski preparati ( Lyobif, Flonivil BS)
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**Laksansi**
Laksansi koji su omeksivaci stolice
Laksansi koji deluju zapreminom
Nadrazajni laksansi
Drugi laksansi koji se jos koriste
- Ricinusovo ulje - Antrahinonske
droge (list sene)
- Bisakodil
- Biljna vlakna
(citrucel, metamucil
- Agar (bozen tablete) - Soni laksansi
(MgSO4, Mg(OH)2,
Na2SO4
- PoliEtilenGlikol
(salinska lavaza
creva)
- Tecni parafin -Dioktil-Na-Sulfosukcinat - Glicerol
- Laktuloza -Cisaprid
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Beta-laktamski antibiotici(penicilini, cefalosporini, monobaktami i karbapenemi)
PENICILINI
1. benzilpenicilini i srodni penicilini (prirodn, uskospektralni)-parenteralno
benzilpenicilin(penicilin G)-suvi-kristalni, rastvorljive Na i K solidepo penicilini:prokain-benzilpenicilin (JUGOCILIN) im, benzatin-benzilpenicilin (PANAPEN)im,benzilpenicilin+prokain-benzilpenicilin
-oralnipenicilin V (fenoksimetilpenicilin) CLIACIL
2. penicilini otporni prema penicilinazi (antistafilokokni)oksacilini (oksacilin, kloksacilin, dikloksacilin, nafcilin), meticilin
3. penicilini proirenog spektra dejstva (aminopenicilini, irokospektralni)amoksicilin, ampicilin PENTREXYL, pivampicilin, metampicilin
4. antipseudomonasni (karbenicilini i ureidopenicilini)azocilin, mezocilin, piperacilin PIPRIL, tikarcilin
INHIBITORI BETA-LAKTAMAZAklavulanska kiselina, tazobaktam, sulbaktamkombinovani preparati: AMOKSIKLAV, PANKLAV=kk+amoksicilin,SULTAMICIN=sb+ampicilin,TAZOCIN=tzb+piperacilin
MONOBAKTAMI (aztreonam) I KARBAPENEMI (imipenem)
*Th penicilinskog oka:1.Adr im 1 mg (10g/kg kod dece) ili iv 10 puta manje, ponovljati pp svakih 10-20 min,obicno 4-5 puta2. Antihistaminik iv (prometazin,difenilhidramin,hlorpiramin) potom oralno tokom 48h,3. Aminofilin 250-500 mg iv polako, ako dominira bronhospazam,4. Kortikosteroid im, dejstvo nastupa za 45 min.
CEFALOSPORINIPrva generacija
Cefaleksin PALITREXpos, Cefazolin GALACEF, Cefadroksil DURACEFposDruga generacija
Cefaklor ALFACETpos, Cefamandol MANDOL, Cefoksitin MEFOXIN, CefuroksimNILACEF, ZINACEF, Cefprozil CEFZILpos
Treca generacijaCefotaksim TOLYKAR, CEFAPAN, Ceftriakson LONGACEPH, AZARAN,ROCEPHIN, Cefpodoksim OBRELANpos, Ceftazidim FORTUM, FORCAS,Cefoperazon CEFOBID, Ceftibuten CEDAXpos
etvrta generacijaCefpirom CEFROM, Cefepim MAXIPIME, MAXICEF
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OSTALI INHIBITORI SINTEZE EL. ZIDAVankomicin, Teikoplanin, Fosfomicin, Bacitracin, Cikloserin
AMINOGLIKOZIDI prvenstveno za g- bakterijeStreptomicin, Gentamicin GENTAMICIN, GARAMICIN, Amikacin AMIKACIN,Netilmicin NETROMYCIN, Tobramicim TOBREX, Kanamicin,NEODEKSACIN=dexametazon+neomicin
ANTITUBERKULOTICIIzoniaazid IZONIAZID, Rifampicin RIFTAN, RIFAMOR, StreptomicinSTREPTOMISIN-SULFAT inj., Etambutol MYAMBUTOL
LEKOVI PROTIV LEPREDapson, Rifampicin, Klofazimin
Hloramfenikol CHLORAMFENIKOL
TETRACIKLINI per osPrirodni: Tetraciklin AMRACIN, Oksitetraciklin, HlortetraciklinModifikovani: Doksiciklin DOVICIN,VIBRAMICIN, Demeklociklin, Metaciklin
MAKROLIDIEritromicin ERITROMICIN, Azitromicin HEMOMYCIN, Roksitromicin RUNAC,ROXIMISAN, Klaritromicin KLACID, Midekamicin MACROPEN, SpiramicinROVAMICIN, Telitromicin KATEK
LINKOZAMINIKlindamicin KLINDAMICIN, Linkomicin LINCOHEM, LINCOCIN
FUZIDINSKA KISELINA
AB ISKLJUCIVO ZA LOKALNU PRIMENUPolimiksin, Bacitracin, Neomicin, Bacitracin+ Neomicin =BIVACYN
SULFONAMIDI (Antifolati)Sulfagvanidin, Sulfadiazin-srebro SANADERM, Sulfasalazin,Sulfametoksazol+Trimetoprim=Kotrimoksazol BACTRIM, BIOPIRIN, TRIMOSAZOL,TRIMOSUL, BACTIMOL 5-aminosalicilna kiselina 5-ASA
FLUOROHINOLONICiprofloksacin CIPROCINAL, Norfloksacin, Fleroksacin QUINODIS, OfloksacinVISIREN
UROANTISEPTICINitrofurantoin, Metenamin-mandelat, Hinoloni: Nalidiksinska kis, Pipemidna kis,Oksolonska kis.
ANTIGLJIVINI LEKOVI...ANTIVIRUSNI LEKOVI...ANTIMALARICI...AMEBICIDI...ANTIPARAZITNI LEKOVI...
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==Antibiotici==**Penicilini**
Prirodni penicilini
Penicilaza rezistentni penicilini
Penicilini prosirenog spektra - Aminopenicilini
Penicilini protiv pseudomonasa
- Benzilpenicilin (penicilin G) par ent
- Benzatin-benzilpenicilin
- Prokain-benzilpenicilin
- Klemizol-benzilpenicilin
- Fenoksipropilpenicilin (propicilin)
- Fenoksimetilpenicilin (penicilin V)
- Feneticilin
- Benzilpenicilin+prokain-
benzilpenicilin (bipenicilin, jugocilin)
per os :
Depo preparati :
- Oksacilin - Kloksacilin - Dikloksacilin - Flukoksacilin
- Ampicilin - Amoksicilin - Pivampicilin - Metampicilin
- Karbenicilin - Karfecilin - Ureidopenicilini :
- Mezlocilin- Azlocilin - Piperacilin
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Monobaktami- Aztreonam
Karbapenemi- Imipenem
**Karbapenemi i Monobaktami**
**Glikopeptidi**- Vankomicin - Teikoplanin
**Makrolidi**- Eritromicin - Linkozamini (Linkomicin, Klindamicin)
- Fuzidinska kiselina (stanicid)
- Azitromicin - Klaritromicin
**Streptogramini**- Kvinupristin - Dalfopristin
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**Cefalosporini**
Prva generacija
Druga generacija
Treca generacija
Cetvrta generacija
- Cefazolin par ent - Cefaleksin per os
- Cefuroksim par ent - Cefaklor per os
- Cefotaksim par ent - Cefiksim per os
- Ceftriakson par ent
- Ceftazidim par ent
- Cefpirom par ent
- Cefepim par ent
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**Aminoglikozidi**- Streptomicin
- Gentamicin
- Tobramicin
- Amikacin
- Neomicin
- Kanamicin
**Tetraciklini**- Tetraciklin
- Oksitetraciklin
- Metaciklin
- Doksiciklin
**Sulfonamidi**- Sulfadiazin (opste infekcije)
- Sulfadimetoksin (depo preparat)
- Sulfacetamid (za lokalnu primenu)
- Sulfafurazol (za mokracne infekcije)
- Sulfagvanidin (za crevne infekcije)
- Salazosulfapiridin (za crevne infekcije)
Kotrimoksazol (baktrim) =
trimetoprim+sulfometoksazol
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**Uroantiseptici**1) Nitrofurantoin
2) Metamin-mendelat
3) Hinoloni
Nalidiksinska kiselina
Pipemidinska kiselina
Fluorohinoloni
Ofloksacin
Nofloksacin
Ciprofloksacin
Flourohinoloni trece generacije
- Levofloksacin - Lomefloksacin
**Antibiotici za lokalnu primenu**
- Polimiksin - Bacitracin - Neomicin
www.belimantil.info
**Amebicidi**
Tkivni Luminalni
- Emetin i Dihidroemetin
- Metronidazol
- Hlorokin
- Jodokinol i Kliokinol
- Diloksanid-furoat
- Neki antibiotici :
- Tetraciklini
- Eritromicin
- Paromomicin
**Antituberkulotici**
- Rimfampicin
- Izoniazid
- Etambutol
- Etionamid
- Pirazinamid
Alternativni antituberkulotici :
- Kapreomicin
- Cikloserin
- Para amino salicilat (PAS)
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**Antimikotici**
Antimikotici za sistemsku primenu
Antimikotici za lokalnu primenu
- Amfotericin B
- Flucitozin
- Derivati imidazola ( Mikonazol, Ketokonazol)
- Grizeofulvin (zbog teratogenosti i kancerogenosti umesto njega koristimo
Itrakonazol i Terbinafin)
- Flukonazol
- Nistatin
- Tolnaftat
- Derivati imidazola za lokalnu primenu (Mikonazol, Klotrimazol, Tindazol)
- Natamicin
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**Antivirusni lekovi**
Lekovi protiv Herpesa
Inhibitori proteaze
Inhibitori reverzne transkriptaze
Ostali- Amantadin - Ribavirin - Interferoni
- Indinavir - Ritonavir
Analozi nukleozida : Ne-nukleozidni inhibitori r.t.
- citidina (Zalcitabin, Lamivudin)
- timidina ( Zidovudin, Stavudin)
- inozina (Didanozin)
- Efavirenz
- Aciklovir
- Ganciklovir
- Famciklovir
- Penciklovir
- Valaciklovir
- Foskarnet
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**Antiparazitarni lekovi**
Lekovi protiv skabies-a
Antihelmintici
- Heksahlorcikloheksan
- Benzil-benzoat
- Krotamiton
- Sumpor mast ili alkalni sulfidi
- Albendazol
- Mebendazol
- Niklozamid
- Tiabendazol
- Piperazin
- Pirantel-Pamoat
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ANS.pdfCNS.pdfCNSPharmacology.pdfKVS.pdfAntiaritmici.pdfRespiratorni.pdfGIT.pdfAntibiotici.pdfAntibiotici.pdf