EXAM ABC June 2023 Department of Pharmacology Examples of ABC drug desciptions MF3 2023 No Drug name Pharmacological group (A) 1. Mucolytic 2. Antidote Mechanism of action + Pharmacological effect (B) Depolymerisation of mucoproteins. Secretolytic effect. Restore glutathione storage in case of paracetamol overdose. 1. Acetylcysteine 2. Acetylsalicylic acid 1. Antiplatelet; 2. NSAID 3. Acyclovir Antiinfective Antiviral agent Antiplatelet – irreversible COX1 inhibition, inhibition of thromboxane A2 synthesis; blockade of platelet activation in aggregation phase, antithrombotic effect NSAID - COX2 inhibition, analgesic, anti-fever, anti-inflammatory action Antimetabolite, analogue of guanosine, inhibition of viral DNA polymerase, virustatic action 4. Adrenaline (Epinephrine) Non-selective adrenomimetic 5. Alendronic acid Bisphosphonate 6. Allopurinol Anti-gout agent 7. Alteplase Thrombolytic Direct stimulation of alfa1&2 and beta 1&2 adrenoreceptors. “+” ino, “+” batmo, “+” dromotropic effects, local haemostatic action. Antianaphylaxis action, cardiotonic action, bronchodilatation and vasoconstriction Inhibition of farnesyl pyrophosphate synthase, inhibit of activation of osteoclasts,, antiresorbtive action Inhibits enzyme xanthine oxidase, blockade of synthesis of uric acid uricostatic action Activator of plasminogen. Fibrinolytic effect Indications (C) 1.Acute or chronic bronchitis with productive cough 2. Intoxication with paracetamol 1. Secondary prophylaxis of cerebrovascular and cardiovascular thrombosis 2. Pain, fever Herpes zoster and Herpes simplex virus infections Varicella zoster infections Systemic use: anaphylaxis, cardiopulmonary reanimation (AV blockade) Local use: in combined preparations with local anesthetics Osteoporosis Oncogenic hypercalciemia Comments NSAID – nonsterpoidal antiinflammatory drug In osteoporosis prophylaxis of vertebral and nonvertebral fractures Gout Management of malignancy associated hyperuricaemia Acute coronary syndrome. stroke 1 EXAM ABC June 2023 Department of Pharmacology No Drug name 8. Amiodarone 9. Amitriptyline 10. Amoxicillin (A.) + clavulanic acid (C.) 11. Aripiprazole Pharmacological group (A) Antiarrhythmic Agent (Class III) Non-selective monoamine reuptake inhibitor, tricyclic antidepressant Antiinfective Beta-lactam antibiotics, Penicillins (3rd generation) Atypical antipsychotic drugs Mechanism of action + Pharmacological effect (B) Phase 0 of AP: blockade of sodium ion channels in cardiomyocytes, extending QRS complex; Phase 3 of AP: blockade of potassium ion channels in cardiomyocytes, prolonging QT interval’ Phase 2 of AP: blockade of calcium ion channels in cardiomyocytes. Phase 0 and 4 of AP: blockade of calcium ion channels in SA and AV nodes. Iodine in structure can influent action of thyroid gland antiarrhytmic action Non-selective inhibition of reuptake of monoamines (norepinephrine, serotonine), anticholinergic activity psychomotor weighing down, sedative action, coanalgetic action A. Blockade of bacterial cell wall synthesis, inhibition of transpeptidase, C. inhibitor of beta lactamase A.+C. broad spectrum bactericidal action 5-HT2A antagonist, D2 partial agonist Influence on serotoninergic and dopaminergic receptors of brain cortex and limbic system Antipsychotic and mood stabilizing action Indications (C) Comments Supraventicular (e.g. atrial fibrillation) and ventricular arrhythmias AP – action potential; SA – sinoatrial; AV atrioventricular Depression Neuropatic pain Treatment of infections caused by Gr+ and Grbacteria that are sensitive to this antibacterial agent Some examples: pneumonia, acute otitis, sinusitis, cystitis Psychiatric diseases Example:schizophrenia, bipolar disorder 2 EXAM ABC June 2023 Department of Pharmacology No Drug name Pharmacological group (A) Hypolipidemic agents Mechanism of action + Pharmacological effect (B) Inhibition of hydroxy-3-methyl-glutaryl coenzyme A (HMG-CoA) reductase, blockade of synthesis of cholesterol precursor – mevalonic acid in liver, increases the number of hepatic low-density lipoprotein (LDL) receptors on the cell-surface to enhance uptake and catabolism of LDL, thus lowering plasma lipoprotein and cholesterol levels, hypolipidemic, pleiotropic (e.g. enhancing the stability of atherosclerotic plaques) effects Indications (C) Comments 12. Atorvastatin Dislipidemias Prophylaxis of cardiovascular diseases (primary, secondary) Atropine M-cholinoblocker Non-selective blockade of M cholinoreceptors, „+” crono and dromotropic effects, spasmolytic, secretolytic, prolonged mydriatic actions. Bevacizumab Antineoplastic agent, Recombinant humanized monoclonal IgG1 antibody Binds to vascular endothelial growth factor (VEGF) and inhibits the interaction of VEGF to receptors on the surface of endothelial cells. In the process, it prevents the proliferation of endothelial cells and formation of new blood vessels, anti-blastic action systemic use: a) symptomatic sinus bradycardia, blockade of AV node b) preoperative – to reduce secretion of salivary glands c)antidote in case of poisoning with muscarinecontaining mushrooms and anticholinesterase inhibitors local use (in eye drops): mydriasis and cycloplegia for ophthalmic investigations Neoplasms, e.g. colorectal cancer, breast cancer, lung cancer, renal carcinoma Cholesterolindependent or “pleiotropic” effects of statins involve improving endothelial function, enhancing the stability of atherosclerotic plaques, decreasing oxidative stress and inflammation, and inhibiting the thrombogenic response Mydriatic action is very long (≈7 days) in comparison with tropicamide (≈6-7 hours). 13. 14. Age-related macular degeneration 3 EXAM ABC June 2023 Department of Pharmacology No Drug name Pharmacological group (A) Chemical irritating stimulant laxative Vitamins Vitamin D biologically active form Antiepileptic agent Mechanism of action + Pharmacological effect (B) Directly enhances peristaltic of intestines; additionally has osmotic effect in the colon, laxative effect Nonselective D vitamin receptor (intracellular) agonist. Provides calcium absorption in the GIT and reabsorption from kidney. Regulates Ca2+ homeostasis Indications (C) 15. Bisacodyl 16. Calcitriol 17. Carbamazepine Blocks neuronal voltage-gated sodium (calcium) channels and decreases the excitation. Anticonvulsant action, mood stabilization, analgesic action Ciprofloxacin Synthetic antiinfective Quinolone (fluorquinolone) Inhibition of DNA gyrase, inhibition of synthesis of nucleic acids, bactericidal action 19. Clarithromycin Antiinfective macrolide antibiotic Inhibition of ribosomal protein synthesis. Broad spectrum Bacteriostatic effect 20. Clindamycin Antiinfective lincozamide antibiotic Inhibition of ribosomal protein synthesis. Broad spectrum Bacteriostatic effect Grand mal epileptic seizures, bipolar disorder, neuropathic pain Treatment of infections caused by Gr+ and Gr(mostly Gr-) bacteria that is sensitive to this antibacterial agent Examples: pyelonephritis, bacterial traveller diarrhea Treatment of infections caused bacteria that are sensitive to this antibacterial agent Examples: H. pylori infection, legionellosis Treatment of infections caused bacteria that are sensitive to this antibacterial agent Examples: osteomyelitis, Acne vulgaris, bacterial vaginose Arterial hypertension, Coanalgesia 18. Side effect: pseudomembranous colitis 21. Clonidine Central α2 adrenoreceptor and imidazoline receptor agonist Central presynaptic and postsynaptic α2 receptora and imidazoline receptor stimulation, peripheral blood vessel dilation. Hypotensive effect. Regulates subcortical activity in the brain. Decreases pain impulse transmission in the brain co-analgetic effect Comments Constipation Rickets, osteoporosis prophylaxis Renal osteodystrophy GIT –gastrointestinal tract 4 EXAM ABC June 2023 Department of Pharmacology No Drug name 22. Clopidogrel Pharmacological group (A) antiplatelet agent Mechanism of action + Pharmacological effect (B) ADP (P2Y12 type) receptor antagonist, blocks thrombocyte activation in aggregation phase antithrombotic effect Folate antagonist. T. –dihydrofolate reductase inhibitor, S. – dihydropteroate synthase inhibitor, PABA antagonist Bactericidal effect 23. Co-trimoxazole (combination of sulfamethoxazole (S.) and trimethoprim (T.)) Combined synthetic antimicrobal agent Sulphonilamide + trimetoprim 24. Dabigatran Direct oral anticoagulant (DOAC) Competitive, direct thrombin (II a coagulation factor) inhibitor, antithrombotic action 25. Desmopressin Neurohypophyseal hormone, analog of antidiuretic hormone 26. Dextrometorphan Central acting antitussive 27. Diazepam Anxiolytics of benzodiazepine group Vasopressine-2 (V2) receptor agonist, analog of antidiuretic hormone that affects conservation of water in the kidneys, Antidiuretic action Increasing plasma levels of factor VIII activity in hemophilic individuals and patients with von Willebrand's disease. Antihemorrhagic action NMDA receptor antagonist, sigma 1,2 non-opioid receptor agonit, depress activity of cough center in medulla oblongata antitussive action GABA A allosteric modulator. Non-selective binding to alpha subunit (BZD receptors), enhance affinity of GABA-A receptor to endogenous ligand - GABA, hyperpolarization of cell membrane. long action, anxiolytic, myorelaxant, anti-seizure and hypnotic action Long-term use cause dependence Indications (C) secondary prophylaxis of cerebrovascular and cardiovascular thrombosis Treatment of infections caused bacteria that are sensitive to this antibacterial agent Examples: urethritis, cystitis, acute otitis Prophylaxis and treatment of deep vein thrombosis (DVT) and pulmonary thromboembolism (PATE) 1. Diabetes insipidus, nocturnal enuresis 2. Hemophilia A, von Willebrand disease Comments PABA –paraaminobenzoic acid Non-productive cough Psychiatric and psychoneurotic diseases, e.g. anxiety, For sedation, Seizures GABA –gamma aminobutyric acid BDZbenzodiazepine 5 EXAM ABC June 2023 Department of Pharmacology No Drug name 28. Diclofenac 29. Digoxin 30. Diltiazem Pharmacological group (A) Nonsteroidal antiinflammatory drugs Mechanism of action + Pharmacological effect (B) COX1 and COX2 inhibitor (more selewctive against COX2) inhibition of prostaglandin synthesis, including thromboxane A2 inhibition in platelet antiinflammatory, analgesic, and antipyretic action Indications (C) 1. Antiarrhythmic agent (Class, V) 2. Cardiotonic agent Cardiac glycosides – digitalis glycosides Na+/K+ ATPase (pump) inhibitor, Na+/Ca2+ ion exchange pump (NCX) inhibitors Reflectory increases n. vagus tonuss (due to increased heart output) that cause: Negative chronotropic and dromotropic effects (inhibit AV transmission). Antiarrhytmic action Positive inotropic effect, because in the myocardial cell increases the calcium ion concentration (due to inhibition of Na+/Ca2+ ion exchange) Cardiotonic action Phase 2 of AP: blockade of calcium ion channels in cardiomyocytes, reduce calcium influx ("-" inotropic effect in high doses) Phase 0 and 4 of AP: blockade of calcium ion channels in SA node – reduce heart rate (("-" chronotropic effect); Reduce afterload - reduce oxygen demand in myocard. Dilatate coronary blood vessels – increase oxygen supply to myocard, antianginal action. 1. Supraventricular rhythm disorders (for example atrial fibrillation/flutter) Calcium channel blocker – nondihydropyridines Antiarrhythmic agent (Class, IV) Comments Muscoloskeletal system diseases, e.g. rheumatoid arthritis, osteoarthritis, Short-term mild to moderate acute pain 2. Chronic heart failure Arterial hypertension, Stable angina Vasospastic or Prinzmetal's angina Supraventricular rhythm disorders (for example atrial fibrillation) AP – action potential; SA – sinoatrial; AV atrioventricular Blockade of calcium channels in peripheral blood vessels smooth muscles, reduce peripheral resistace (after load) and reduce blood pressure, antihypertensive effect Phase 0 and 4 of AP: blockade of calcium ion channels in AV node – cause "-" dromatropic effect); antiaarhytmic effect (only in high doses) 6 EXAM ABC June 2023 Department of Pharmacology No Drug name 31. Dobutamine 32. Dopamine Cardiotonic agent Adrenomimetic agent 33. Doravirine 34. Dorzolamide 35. Doxazosin Non-nucleoside RNA-dependent DNA polymerase or reverse transcriptase inhibitor (NNRTIs) Carbonanhidrase inhibitor Alpha1 adrenoblocker 36. Doxorubicine Pharmacological group (A) Cardiotonic agent Adrenomimetic agent Antineoplastic agent Chemotherapy agent Anthracycline antitumor antibiotic Mechanism of action + Pharmacological effect (B) Beta1 adrenoreceptor agonist +" Inotropic effect because of increasing of calcium ion concentration in myocardial cells.Moderate "+" chronotropic effect. Possesses weak beta2 and alpha1 adrenomimetic effect - reduces peripheral vascular resistance (afterload, systolic pressure does not change or increases (increases the cardiac volume) Cardiotonic action Dopamine receptor agonists, beta1, alpha1 adrenoceptor agonist. Effect is dose-dependent (in low doses improves renal microcirculation, in moderate doses cause “+” inotropic effect, in high doses – mostly is vasopressor effect) Cardiotonic effect NNRTI of HIV-1 and inhibits HIV-1 replication by noncompetitive inhibition of HIV-1 reverse transcriptase. Does not inhibit the human cellular DNA polymerases alpha, beta and mitochondrial DNA polymerase gamma Indications (C) Inhibition of carbonanhidrase, decrease intraocular fluid synthesis, reduce IOP. Antiglaucoma effect Blockade of alpha 1B- adrenergic receptors lead to venous and arterial smooth muscle relaxation reduces peripheral resistance (afterload), increase venous capacity (preload) and reduce blood pressure, antihypertensive action Glaucoma Blockade of alpha 1A- adrenergic receptors decreases smooth muscle tone in the prostate, its capsule and bladder, facilitates urination, Urodynamic action Intercalant, topoisomerase II inhibition un free radicals formation break down DNA cytotoxic effect Comments Acute heart failure (myocardial heart attack, heart surgery or septic and cardiogenic shock) Acute heart failure (myocardial infarction, heart surgery and septic cardiogenic shock) HIV infection IOP –intraocular pressure Arterial hypertension Symptomatic treatment of benign prostatic hyperplasia Various treatment of neoplasia (e.g. breast cancer, acute lymphocytic leukemia, etc.) 7 EXAM ABC June 2023 Department of Pharmacology No Drug name 37. Doxycycline 38. Enoxaparine 39. Ethynylestradiol Pharmacological group (A) Antiinfective Antibiotic, Tetracycline Anticoagulant Low molecular weight heparin (LMWH) Female sex hormone, semisynthetic estrogen Mechanism of action + Pharmacological effect (B) inhibiting ribosomal bacterial protein synthesis, broad spectrum bacteriostatic activity side effect: photosensitivity Forms a complex with antithrombin III, increases antithrombin III activity, Indirect inhibition of coagulation factors Xa and IIa antithrombotic effect Alpha and beta estrogen receptor agonist 1. Replaces endogenous hormones estrogen substitution 2. Gonadotropins LH and FSH release feedback inhibition, inhibit follicule maturation and ovulation. Hormonal suppression effect Indications (C) Active against Gr+ and Grmicroorganisms Boreliosis, chlamidiosis Treatment and prevention of venous thromboembolic disease As mono-drug in replacement therapy (after ovarectomy) if there is a primary estrogen hormone deficient or related disorders (vasomotor symptoms caused by menopause) Component of combined oral contraception (COC) 40. Etoricoxib 41. Fluconazole 42. Fludrocortisone Nonsteroidal antiinflammatory drugs Antiinfective Antimycotic agents azole derivatives (2nd generation - triazole derivatives) Mineralocorticoid selective COX2 inhibitor inhibition of prostaglandin synthesis without thromboxane A2 synthesis inhibition of platelet (no effect COX1 the enzyme) antiinflammatory, analgesic, and antipyretic action Demethylase inhibition; inhibits biosynthesis of ergosterol or other sterols, damaging the fungal cell wall membrane and altering its permeability Fungistatic effect Agonist to mineralcorticoid receptors, cause sodium and water reabsorption in distal nephron tubules. Restore electrolyte and water homeostasis. Comments If women has uterus, estrogens could be used only together with progesterone to reduce risk of endometrial cancer. LH – luteinizing hormone FSH – follicle stimulating hormone Muscoloskeletal system diseases, e.g. rheumatoid arthritis, osteoarthritis, inflammatory symptoms of acute gouty arthritis Dermatophytes and Candida (type of yeast) fungal infection of the nails, skin, genital mucous membrane Chronic adrenal gland failure (Addison disease) 8 EXAM ABC June 2023 Department of Pharmacology No Drug name Pharmacological group (A) Anti-tumor (antineoplastic) agent Chemotherapy agent Mechanism of action + Pharmacological effect (B) Pyrimidine antagonist, antimetabolite Inhibit DNA and RNA synthesis in cell cycle S phase Cytotoxic effect 43. Fluorouracil 44. Indications (C) Furosemide Loop diuretics High-ceiling diuretic Potassium wasting diuretics Inhibition of Na+/K+/2Cl- transportier (NKCC2) short acting Promote excretion of sodium, potassium, cloride, magnesium, calcium; reduce excretion of uric acid, acting in ascending part of loop of Henle Diuretic effect Diuretics lower blood pressure initially by reducing plasma and extracellular fluid volume, reduce blood vessels sensitivity to circulating catacholamines. Hypotensive effect + see comments! 45. Gabapentin Antiepileptic agent Gammaaminobutyric acid (GABA) analogue Voltage-gated N-type Ca2+ channels inhibition anticonvulsant, analgesic effect Partial seizure Peripheral neuropathic pain (diabetic neuropathy, postherpetic neuralgia) 46. Gentamycin Anti-infective drug Aminoglycoside antibiotic Inhibition of ribosomal proteīns, broad spectrum, bacteriocidal action. Side effects: ototoxicity, nephrotoxicity 47. Gliclazide Antidiabetic agent Sulphonylureas derivate ATP-dependent potassium channel blocker. By binding to the SUR1 subunit atATP-sensitive (ATPdependent) K+ channel multimer complex, induces K+ channel inhibition. Further depolarization of the beta cell membrane causes Ca2+ channel opening and ↑Ca2+ concentration → ↑insulin secretion (stimulation of secretion is independent of glucose concentration) Hypoglycemic effect Treatment of infections caused by Gr+ and Grbacteria that are sensitive to this antibacterial agent Examples: sepsis, peritonitis Type 2 diabetes mellitus Neoplasms, eg. breast cancer, carcinoma of pancreas, colorectal and gastric cancer Chronic heart failure Edema caused by renal failure or liver diseases Pulmonary, burns and cerebral edema Arterial hypertension Comments Dose depending effect: “ceiling” dose shows max Na+ excretion; if dose is higher than “ceiling” dose only moderate additional effect is observed. Additional “ceiling” dose administration is more effective then just increasing of dose 9 EXAM ABC June 2023 Department of Pharmacology No Drug name 48. Glyceryl trinitrate 49. Goserelin 50. Haloperidol 51. Hydrochlorothiazide Pharmacological group (A) organic nitrates Gonadotropin releasing hormone analogue. Anticancer (antineoplastic) agent Typical antipsychotic Thiazide diuretic, Low-ceiling diuretic Potassium wasting diuretics Mechanism of action + Pharmacological effect (B) NO donors short and fast acting in low doses – venodilatation action (influent preload), in high doses – also arterial dilatation properties (influent afterload), reduce oxygen consumption in the myocardium Coronary dilation activity increases the oxygen supply to the myocardium. Vasodilatation cause reduction of blood pressure Antianginal and hypotensive effect GnRH superagonist, inhibition of secretion of gonadotropins (LH and FSH), depressing of functions of ovaries and testicles. Antiandrogenic, antiestrogenic action D2 blockers, 5-HT2A antagonists, Haloperidol has a strong influence to delusions and hallucinations because of direct central blockade of D2 receptors. Causes efficient psychomotor sedation, which explains the positive impact on mania and other agitation syndromes antipsychotic action extrapyramidal side effects Inhibits Na+/Cl- transporter in nephron distal convoluted tubule; promote the excretion of sodium, potassium, chloride, magnesium, reduce calcium and uric acid excretion, diuretic effect; Reduce blood vessels sensitivity to circulating catacholamines. Additional extrarenal vasodilatating effect, hypotensive effect Diuretical effect is not strong, “low-ceiling diuretic”, the most part of Na+ is reabsorbed. Indications (C) Comments Angina attack, hypertensive crisis with decompensated heart failure Cancers, e.g. prostata cancer, breast cancer Schizophrenia Acute psychotic disorders, e.g. delirium D2- dopamine 2 5HT - serotonine Arterial hypertension 10 EXAM ABC June 2023 Department of Pharmacology No Drug name Pharmacological group (A) monoclonal antibody against tumor necrosis factor alpha (TNFα) biological diseasemodifying antirheumatic drug (b-DMARD), Hypoglycemic agent Insulin analogue, 52. Infliximab 53. Insulin Lispro 54. Isosorbide mononitrate Organic nitrates 55. Isotretionin Vitamins Synthetic retinoid 56. Labetalol Alpha-1 and Betanon-selective adrenoblocker 57. Lamotrigine Antiepileptic Mechanism of action + Pharmacological effect (B) Inhibit TNF-alpha immunosuppressive action Indications (C) Rapid onset and short-acting insulin analogue. Stimulates tyrosin kinase-dependent insulin receptors, activates GLUT4 transporter and glucose transport into the cell. Inhibits gluconeogenesis. Hypoglycemic effect. NO donors long-acting in low doses – venodilatation action (influent preload), in high doses – also arterial dilatation properties (influent afterload), reduce oxygen consumption in the myocardium Coronary dilation activity increases the oxygen supply to the myocardium. Vasodilatation cause reduction of blood pressure Antianginal and hypotensive effect Retinoic acid receptor (intracellular) agonist. Comedolytic and anti-inflammatory action Teratogenic action Relaxation of smooth muscles of veins and arteries, reduce peripheral resistance (reduce afterload), increase capacity of veins (reduce pre-load) and reduce blood pressure. Hypotensive effect Blocks neuronal voltage-gated sodium and calcium channels in neurons, decreases the excitation. Anticonvulsant action, mood stabilization Diabetes mellitus type I Diabetes mellitus type II in decompensation stage Comments Rheumatoid arthritis, spondylitis, psoriatic arthritis, ulcerative colitis, Crohn’s disease Prevention of angina attacks Severe Acne forms Hypertonic crisis Hypertension in pregnancy Generalized epilepsy Bipolar disorder 11 EXAM ABC June 2023 Department of Pharmacology No Drug name 58. Latanoprost 59. Levodopa (L.)/ Benserazide (B.) combined antiparkinsonian agent 60. Levonorgestrel female sex hormones, synthetic gestagens 61. Lidocaine Pharmacological group (A) Prostaglandin F2 alpha analogs Mechanism of action + Pharmacological effect (B) PGF2 alpha receptor agonist the main mechanism of action is increased uveoscleral outflow, reduces intraocular pressure Antiglaucoma action L. – dopamine precursor, stimulates dopamine (D) receptors. B. – DOPA decarboxylase inhibitor Treatment of extrapyramidal disorders 1. Inhibition of gonadotropin LH and FSH release (feedback). Prevents follicle maturation and ovulation. 2.Inhibit prolypheration stage, increase viscosity of cervical mucus, inhibits motility of uterus, hormonal suppression effect Local anesthetics, amide type Antiarrhythmic Agent (Class Ib) Blockade of sodium ion channels (stabalize of membrane), inhibition of nerve impulse conduction in sensitive nerve fibers, anesthetic effect 62. Loperamide opioid antidiarrheal agent 63. Loratadine histamine-negative agent of 2nd generation Phase 0 of AP: blockade of sodium ion channels in cardiomyocytes; QRS complex do not changed; Phase 3 of AP: activation of potassium ion channels in cardiomyocytes, QT interval is shortened or not changed antiarrhytmic action peripheral μ-opioid receptor agonist in the colon, inhibits gastrointestinal motility, reduce water and electrolyte loss. antidiarrheal effect H1 receptor pharmacodynamic antagonist, decreases capillary permeability anti-allergic effect 64. Macrogol Osmotic laxative Increase amount of fluid in intestines, laxative action Indications (C) Comments Open-angle glaucoma Ocular hypertension Parkinson’s disease, parkinsonism (except antipsychotic agents’ – induced) 1. emergency contraception, 2. oral birth control (in combinations with other agents or as monopreparation) Locally: L. all types of local anesthesia AP – action potential; SA – sinoatrial; AV atrioventricular Systemic use: L. ventricular arrhythmia Acute diarrhoea allergic rhinitis, conjunctivitis, urticaria, hay fever, allergic skin diseases, angioedema (Quincke’s edema) Constipation 12 EXAM ABC June 2023 Department of Pharmacology No Drug name Pharmacological group (A) Osmotic diuretic 65. Mannitol 66. Mesalazine 67. Metformin 68. Methotrexate Imunosuppressant Antimetabolite DMARD Antitumour agent 69. Metoclopramide Antiemetic and gastrokinetic agent Local antiinflammatory agent, 5-aminosalicylic acid (5-ASA) Hpoglycemic agent Biguanid Mechanism of action + Pharmacological effect (B) Increase blood plasma osmolarity, enhance water transport from tissues and organs (also brain, cerebrospinal fluid and eyes) to interstitial compartment and blood plasma, increase water excretion via kidneys. Anti-edema, diuretic action. Reduce intraocualar pressure. Antiglaucoma action. Prostaglandin synthesis inhibition, inflammatory cytokines synthesis inhibition, anti-inflammatory effect and immunosupresive effect Indications (C) aMP-depending proteinkinase induction, gluconeogenesis inhibition in the liver, indirectly promoting GLUT4 expression, reduce insulin resistance in tissues hypoglycaemic effect purine antimetabolite dihydrofolate reductase inhibition additionaly promote accumulation of adenosine immunosuppressive, anti-proliferative, antiinflammatory action D2 receptor antagonist, M-cholinomimetics Type 2 diabetes mellitus Polycystic ovary syndrome inhibition of vomiting center trigger zone dopamine receptors, antiemetic activity gastrointestinal dopamine negative and cholinopositive effect, promotes motility in the upper gastrointestinal tract gastrokinetic effect Comments Cerebral oedema Glaucoma exacerbation Acute renal failure Ulcerative colitis Rheumatoid arthritis Psoriasis Lymphocytic leukemia supportive treatment DMARD – disease modifying antirheumtic drug Chemotherapy and radiation - induced nausea and vomiting Migraine 13 EXAM ABC June 2023 Department of Pharmacology No Drug name 70. Metoprolol Pharmacological group (A) Beta1-adrenoblocker (cardioselective) Antiarrhythmic Agents (Class II) Mechanism of action + Pharmacological effect (B) selective blockade of beta1 adrenoreceptors „-“ ino, chronotropic (reduce oxygen demand in myocard) effects, „-“ dromotropic effect, reduce secretion of renin. Phase 2 of AP: decrease influx of calcium ions in cardiomyocytes. Phase 0 and 4 of AP: decrease influx of calcium ions in SA and AV nodes. 71. Diazepam 72. Montelukast 73. Morphine 74. Nifedipine Anxiolytics of benzodiazepine group Leukotriene receptor antagonist (antileukotriene) Opioid Dihydropiridine calcium channels blockers – see Amlodipine cardiodepressive, antiarrytmic, hypotensive effects GABA A allosteric modulator. Non-selective binding to alpha subunit (BZD receptors), enhance affinity of GABA-A receptor to endogenous ligand - GABA, hyperpolarization of cell membrane. long action, anxiolytic, myorelaxant, anti-seizure action Leukotriene receptor (CysLT1) antagonist, prevention of bronchoconstriction, anti-allergic, antiinflammatory effect Mu (OP3), delta (OP1), kappa (OP2) opioid receptor agonist, spinal and supraspinal analgesia, analgesic effect Could cause dependence Vasoselective blockade of calcium channels, coronary blood vessels dilatation (increase oxygen supply to myocard) arterial vasodilatation, lowers heart after-load (reduce oxygen demand in myocard), hypotensive effect Side effect: peripheral edema Indications (C) Comments Arterial hypertension Chronic heart disease (CHD) Coronary artery disease (CAD) Atrial fibrillation prophylaxis of migraine AP – action potential; SA – sinoatrial; AV atrioventricular For sedation, Seizures Anxiety disorders GABA –gamma aminobutyric acid BDZbenzodiazepine Mild to moderate asthma Prophylaxis, Allergic rhinitis Severe pain MONA algorithm MONA algorithm – pre-hospital stage of acute coronary syndrome management (M – morphine, O – oxygen, N – nitrates, A – antiplatelet) Coronary artery disease (CAD) Stable angina Vasospastic angina Arterial hypertension 14 EXAM ABC June 2023 Department of Pharmacology No Drug name Pharmacological group (A) Non-selective adrenomimetic Mechanism of action + Pharmacological effect (B) Direct stimulation of alfa1&2 and beta 1 adrenoreceptors. “+” inotropic effects, cardiotonic action and vasoconstriction suppresses gastric acid secretion by inhibition of the H+/K+-ATPase in parietal cells antisecretory effect 75. Noradrenaline (norepinephrine) 76. Omeprazole Proton pump inhibitor 77. Ondansetron Antiemetic agent Serotonin (5-HT3)-receptor antagonist area postrema antiemetic effect 78. Oxytocin Neuropituitary hormone 79. Paclitaxel 80. Pancreatin Anticancer agent Taxanes Gastrointestinal agent; Enzyme Digestant 81. Paracetamol Non-opioid analgesic Oxytocin and vasopressin receptor agonist. Dose-depending rhythmic or spastic contractions of myometrium, Stimulates smooth muscle to facilitate ejection of milk from breasts uterotonic effect Inhibition of microtubules depolymerisation, inhibition of mitosis, cytotoxic action Pancreatic enzymes contain the active ingredient pancrelipase. Pancrelipase provides a replacement for digestive enzymes secreted by the pancreas with active porcine derived lipases, proteases and amylases to catalyze the hydrolysis of (1) fat into glycerol and fatty acids, (2) proteins into peptides and amino acids, and (3) starch into dextrins and sugars Prostoglandin H2 synthases inhibitor, prostaglandin synthesis inhibition antipyretic, analgesic effect Indications (C) Comments Acute hypotension, cardiogenic shock Duodenal and gastric ulcer Gastroesophageal reflux disease H. pylori infection Prevention of NSAID provoked gastric and duodenal ulcer Chemotherapy and radiation - induced nausea and vomiting Postoperative nausea and vomiting prophylaxis and treatment Induction of labor Postpartum hemorrhage Termination of pregnancy Lactation stimulation ATP - adenosine triphosphatase Cancers, e.g. breast cancer, ovarian cancer Exocrine pancreatic insufficiency Pain (Mild to Moderate) Fever 15 EXAM ABC June 2023 Department of Pharmacology No Drug name 82. Paroxetine 83. Perindopril Pharmacological group (A) Antidepressant Selective serotonin reuptake inhibitor (SSRI) Anxiolytic agent Angiotensinconverting enzyme (ACE) inhibitors 84. Phenylephrine Adrenomimetic agent Decongestant M-cholinomimetic 85. Pilocarpine 86. Povido-iodine Antiseptic agent Halogen 87. Prednisolone Glucocorticoids Systemic Mechanism of action + Pharmacological effect (B) Selectively inhibits reuptake of serotonin (5-HT) into neurons Antidepressive and anxiolytic effect ACE inhibition blocks angiotensin II and aldosterone formation. (cardiovascular remodelling properties). Dilatation of veins (reduce pre-load) and dilatate arteries (reduce after load) Peridopril is biologically neactive form or pro-drug hypotensive effect promote K+ retention in organism, ACE-I side effects: dry cough Stimulation of alpha 1 receptors hipertensive, mydriatic , vasoconstrictive action Indirect induction of bradycardia Improve outflow of intraocualr fluid, reducē IOP, miotic action, antiglaucoma action, secretogenous action Cytoplasmic and membrane component oxidation, protein denaturation, bactericide, fungicide, virucidal effect 1. Rapid membrane-stabilizing effects (stabilization of lysosomes and mast cells); 2.Slow genomic effects, intracellular corticosteroid receptor activation (indirect inhibition of phospholipase, direct COX2 inhibition) 3. Activator protein AP1 and nuclear factor kappa NFkB inhibition, depression of activation of T lymphocytes anti-inflammatory, antioedema, antialergical, anti - shock immunosuppressive effect side effect: jatrogenic Cushing syndrome Indications (C) Comments Depression Obsessive Compulsive Disorder Panic, anxiety disorders Phobias Arterial hypertension, congestive heart failure active form perindoprilate Hypotension Mydriasis induction, Acute rhinitis Glaucoma Xerostomia Antiseptic processing of the skin and mucous membrane, Wounds and burns cure, Bacterial, and mycotic, viral skin and mucous membranes infections Collagen disease, rheumatic diseases, endocrine disorders, (acute adrenal insufficiency), allergic condition (asthma, contact dermatitis), disorder of skin 16 EXAM ABC June 2023 Department of Pharmacology No Drug name 88. Procainamide Pharmacological group (A) Antiarrhythmic agent (Class Ia) Membrane stabilizer 89. Propofol Non- inhalation general anesthetics 90. Propranolol Non-selective beta1 and beta2 adrenoblockers Antiarrhythmic Agents (Class II) 91. Quetiapine Atypical antipsychotic drugs 92. Rivaroxaban Direct action oral Anticoagulant (DOAC) 93. Rocuronium N-cholinoblocker Non-depolarizing miorelaxant Mechanism of action + Pharmacological effect (B) Sodium channel blockade by extending action potential antiarrhythmic effect Phase 0 of AP: blockade of sodium ion channels in cardiomyocytes; increase QRS complex Phase 3 of AP: blockade of potassium ion channels in cardiomyocytes, QT interval prolongation antiarrhytmic action GABAa allosteric modulator, sedatives, hypnotic, and anesthesia induced effect „-“ ino, chronotropic (reduce oxygen demand in myocard) effects, „-“ dromotropic effect, reduce secretion of renin, non-selective blockade of beta1 and beta2 adrenoreceptors Phase 2 of AP: decrease influx of calcium ions in cardiomyocytes. Phase 0 and 4 of AP: decrease influx of calcium ions in SA and AV nodes cardiodepressive effect, antiarrhytmic, hypotensive effect 5-HT2A antagonist, D2 antagonist Influence on serotoninergic and dopaminergic receptors of brain cortex and limbic system Antipsychotic and mood stabilizing action Selectively inhibits factor Xa Antitrombotic effect N-cholinoreceptor antagonism, cause neuromuscular blockade Indications (C) Comments Atrial and ventricular arrhythmias AP – action potential; SA – sinoatrial; AV atrioventricular General anesthesia Procedural sedation Sedation for a mechanically ventilated patients Arterial hypertension. Arrytmias (atrial fibrillation) Thyreotoxic crisis, prophylaxis of migraine GABA –gammaaminobutyric acid AP – action potential; SA – sinoatrial; AV atrioventricular Psychiatric diseases (e.g. depression, anxiety) Example:schizophrenia, bipolar disorder Prophylaxis and treatment of deep vein thrombosis (DVT) and pulmonary thromboembolism (PATE) Miorelaxation for surgery 17 EXAM ABC June 2023 Department of Pharmacology No Drug name 94. Salbutamol 95. Selegiline 96. Sitagliptin 97. Spironolactone Pharmacological group (A) Selective beta2adrenergic agonist Anti-parkinsonism agent Hypoglycemic (antidiabetic) agent Mineralcorticosteroid (aldosterone) receptor antagonist Potassium sparing diuretics 98. Sumatriptane Antimigraine agent 99. Tiotropium M cholinoblocker Mechanism of action + Pharmacological effect (B) Short-term beta2 adrenergic receptor Stimulation, reduction of intracellular calcium concentration, Bronchodilator, tocolytic effect MAO B inhibition, decrease extrapyramidal symptoms Indications (C) dipeptidylpeptidase 4 (DPP4) inhibition, insulin secretagogues, hypoglycemic action Blocks aldosterone receptors in kidney, in collecting tubule Blocks aldosterone receptors in the myocardium (hearts) and vessels 1. weak diuretic effect 2. antifibrotic effects, 3. anti-androgen effects 5-HT1d agonist, 5HT1b partial agonist Vasoconstriction of meningeal blood vessels Analgesic effect M1-3-cholinoreceptor antagonist, bronchodilatation, antisecretory action GPIIb/IIIa receptor antagonist, blockade of platelet activation in agregation phase. Antithrombotic effect Type 2 diabetes mellitus Complications of fibrinolytic therapy. Adjuvant to hemophillia management Treatment and prophylaxis of drug-induced extrapyramidal disorders Parkinsonism (druginduced) 100. Tirofiban Antiplatelet 101. Tranexamic acid Hemostatic agent Inhibition of plasminogen activation, antifibrinolytic action 102. Trihexyphenidyl Central M and N cholinoreceptor blocker with poor N cholinoblocking properties Blocks M and N cholinergic receptors in nigrostriatal system Reduces tremor, rigidity and bradykinesia that is characteristics of Parkinson disease Reduce extrapyramidal symtoms Comments Asthma Chronic obstructive pulmonary disease Uterine hypertonia Parkinson disease Heart failure Hypertension Primary aldosteronism Acne vulgaris. Hirsutism. Alopecia (in women) Acute migraine (migraine attack) Bronhial asthma, COPD Acute coronary syndrome 18 EXAM ABC June 2023 Department of Pharmacology No Drug name 103. Valproic acid Pharmacological group (A) Anti-epileptics 104. Valsartan Angiotensin II receptor blocker 105. Vancomycin antiinfective Antibiotic Glycopeptide 106. Verapamil Calcium channel blocker, nondihydropyridine Antiarrhythmic agent (IV class) Mechanism of action + Pharmacological effect (B) Blocks voltage-gated CNS sodium (Na+) and calcium (Ca2+) channels in neurons, inhibit GABA transaminase Inhibits excitation Anticonvulsant, mood-stabilizing action Teratogenic action Blocks angiotensin AT1 receptors, reduce synthesis of aldosterone (cardiovascular remodelling properties). Dilatation of arteries (reduce after load) and dilatate veins (reduce pre load) hypotensive effect, antifibrotic effect Inhibits bacterial cell wall synthesis by blockade of Dalanyl-D-alanyl (transglycosydation stage), narrow spectrum bactericidal activity Phase 2 of AP: blockade of calcium ion channels in cardiomyocytes, reduce calcium influx pronounced "-" inotropic effect) Phase 0 and 4 of AP: blockade of calcium ion channels in SA node – reduce heart rate (("-" chronotropic effect); Indications (C) Comments Epilepsy Bipolar disorder Migraine prophylaxis Hypertension Chronic heart failure Gram-positive cocci, including MRSA Cl. Dificille (per os) Angina pectoris (stable, vasospastic) Paroxysmal supraventricular tachycardia, e.g. atrial fibrillation AP – action potential; SA – sinoatrial; AV atrioventricular Reduce afterload - reduce oxygen demand in myocard. Dilatate coronary blood vessels – increase oxygen supply to myocard, antianginal action. Blockade of calcium channels in peripheral blood vessels smooth muscles, reduce peripheral resistace (after load) and reduce blood pressure, antihypertensive effect Phase 0 and 4 of AP: blockade of calcium ion channels in AV node – cause "-" dromatropic effect); antiaarhytmic effect 19 EXAM ABC June 2023 Department of Pharmacology No Drug name 107. Warfarin 108. Xylometazoline 109. Zolpidem Pharmacological group (A) Anticoagulant K vitamin antagonist adrenomimetic agent, nasal decongestant Hypnotic agent Non-benzodiazepine Benzodiazepine (BZD) analogue Mechanism of action + Pharmacological effect (B) Vitamin K antagonist, Inhibits Vitamin K epoxide reductase by this inhibiting synthesis of vitamin K-dependent clotting factors II, VII, IX and X anti-thrombotic action Local α1 and α2 postsynaptic adrenoreceptor agonist. Vasoconstrictive effect GABA A allosteric modulator. Selective binding to alpha 1 subunit (BZD receptors), enhance affinity of GABA-A receptor to endogenous ligand - GABA, hyperpolarization of cell membrane. Hypnotic action Indications (C) Comments Prophylaxis and treatment of deep vein thrombosis (DVT) and pulmonary thromboembolism (PATE) Acute rhinitis Insomnia 20