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Revision of Parasympathomimetics
Answer the following questions:
1-Ennumerate the therapeutic uses of choline esters mentioning examples of the drugs used.
2-Ennumerate the therapeutic uses of muscarinic agonists (parasympathomimetics) mentioning examples of the drugs used.
3-Give a brief account on "myasthenia gravis".
4-Compare between myasthenic crisis and cholinergic crisis.
5-Compare between physostigmine and neostigmine as regards: source, chemistry, actions, and uses.
6-Give an account on acute organophosphorous toxicity as regards: causes, manifestations, and treatment.
7-Give reason (explain):
A-Atropine should be given before neostigmine in diagnosis of myasthenia gravis.
B-Atropine reverses the hypotensive action of acetylcholine large dose, but abolishes the hypotensive action of methacholine large dose.
C-Oximes should be used as early as possible (within 12 hours) in treatment of acute organophosphorous toxicity.
D-Edrophonium is used in diagnosis and not in treatment of myasthenia gravis.
E-In treatment of acute curare toxicity we use neostigmine or edrophonium but not physostigmine.
F-Edrophonium is preferred to neostigmine in differentiation between myasthenic crisis and cholinergic crisis in myasthenia gravis-treated patients.
G-Muscarinic agonists as carbachol and neostigmine are contraindicated in obstructive retention of urine.
H-Muscarinic agonists are contraindicated in thyrotoxicosis.
I-Carbachol and bethanechol have much longer duration of action compared to acetylcholine.
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Revision of muscarinic antagonists
Questions about muscarinic antagonists
Answer the following questions:
1-Enumerate 6 therapeutic uses of atropine, and mention 1 atropine substitute for each use (if available). 2-Give an account on "acute atropine toxicity". 3-Classify synthetic atropine substitutes, mention at least 2 examples for each group. 4-Compare between atropine and hyoscine as regards: chemistry- actions-indications. 5-Mention briefly the adverse effects of atropine. 6-What are the contraindications of atropine? 7-Give reason: A-Atropine should be given before neostigmine in diagnosis of myasthenia gravis. B-Atropine may cause initial transient bradycardia if injected I.V. C-Large and toxic doses of atropine cause "atropine flush". D-Hyoscine is preferred to atropine as "pre-anaesthetic medication". E-Rabbits are tolerant to atropine. F-Ipratropium has replaced atropine in prophylaxis against bronchial asthma. G-Tropicamide is used instead of atropine in "fundus examination". 8-Complete: A-Atropine, hyoscine, and atropine substitutes are absolutely contraindicated in ------- and -------. B- -------- and ------- are atropine substitutes used in prophylaxis of bronchial asthma. C- --------- is the drug of choice in prophylaxis of motion sickness. D-Pirenzepine and telenzepine are selective ----- antagonists used in treatment of ---------. E-Synthetic antiparkinsonian atropine substitutes include ------ and -----.
F- ------- is a selective M3 antagonist used in treatment of ---------.
G- ---------- is a synthetic atropine substitute used in hypertrophic pyloric stenosis.
Revision on Endocrine Pharmacology
Give an account on:
1-Insulin: mechanism of action-indications-adverse effects-preparations.
2-Sulphonylureas: mechanism of action-indications-drug interactions-adverse effects-contraindications.
3-Metformin (Biguanides): actions-indications-adverse effects –contraindications.
4-Diabetic Ketoacidosis (DKA): causes-manifestations-treatment.
5-Thyroid hormones: preparations-indications.
6-Thioamides (Thiourea derivatives): mechanism of action-indications-adverse effects.
7-Radioactive Iodine: types (I131 and I132)-indications-toxicity-contraindications.
8-Iodide: indications (antithyroid + saline expectorant) – adverse effects.
9-Glucocorticoids: preparations-indications-adverse effects-contraindications-precautions during prolonged use.
10-Estrogen: indications-adverse effects –contraindications-drug interactions.
11-Oral contraceptives: mechanism of action-adverse effects-contraindications-methods.
12-Classify agents affecting Ca2+ homeostasis and mention their effect on serum Ca2+.
Explain (Give reason):
1-Insulin is ineffective orally.
2-Metformin is a "euglycemic" not a hypoglycemic drug.
3-Sulphonylureas as glibenclamide may cause hypoglycemia in overdoses.
4-Metformin is contraindicated in COPD.
5-Patients treated with thioamides should do frequent blood count.
6-Thioamides have delayed onset of action.
7-Propylthiouracil is useful in thyrotoxic crisis.
8-Radioactive iodine is contraindicated in young patients.
9-Propranolol is the preferred β-blocker in thyrotoxic patients.
10-Iodides as Lugol's iodine have rapid onset of action.
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11-Glucocorticoids should never be stopped abruptly following long-term use. 12-The dose of prescribed glucocorticoids should be increased during stress. 13-The diet of patients treated with glucocorticoids should be high in proteins, Ca2+, and K+ and low in Na+. 14-ACTH has advantages over glucocorticoids as anti-inflammatory agent. 15-Prednisone and cortisone should be given systemically and not topically. 16-Triamcinolone is preferred to cortisol in hypertensive patients suffering from inflammatory conditions. 17-Asthmatic patients receiving beclomethasone inhalation are advised to perform mouth wash after use of the inhaler. 18-Steroid hormones have a lag period (delayed onset) compared to polypeptide hormones. 19-Thiazide and loop diuretics are better avoided in patients treated with glucocorticoids. 20- A.D.H. is used in treating hemorrhage due to esophageal varices.
Answer the following MCQs:
1-Which of the following hormones acts through a cytoplasmic receptor:
A-Insulin.
B-Vasopressin.
C-Calcitriol (Vitamin D).
D-ACTH.
2-All of the following hormones are polypeptides Except: A-Cortisol.
B-Glucagon.
C-Oxytocin.
D-T.S.H.
3-Gynecomastia can be caused by the following drugs Except:
A-Chlorpromazine.
B-Cimetidine.
C-Bromocriptine.
D-Metoclopramide.
4-Bromocriptine is classified as:
A-D2 Agonist.
B-D2 Antagonist.
C-Both D1 and D2 antagonist.
D-Has no action on D receptors.
5-T.S.H. exerts the following actions Except:
A-Increases vascularity.
B-Inhibits proteolysis of thyroglobulin.
C-Induces hyperplasia and hypertrophy of thyroid gland.
D-Promotes iodide trapping.
6-Liothyronine (L-T3) is preferred to L-Thyroxine (L-T4) in:
A-Endemic goiter.
B-Cretinism.
C-Papillary thyroid carcinoma.
D-Myxedema coma.
7-Which of the following antithyroid drugs inhibits peripheral conversion of thyroxin into triiodothyronine:
A-Propylthiouracil.
B-Methimazole.
C-Carbimazole.
D-Radioactive iodine.
8-Lugol's iodine is used in hyperthyroidism:
A-As long term definitive monotherapy.
B-Preoperatively for 10-15 days.
C-Postoperatively for 10-15 days.
D-As adjuvant to carbimazole as long term therapy.
9-The aim of iodide therapy before subtotal thyroidectomy is:
A-To render the patient euthyroid.
B-To restore the iodine content of the gland.
C-To inhibit peripheral conversion of thyroxine into triiodothyronine
D-To reduce friability and vascularity of the gland.
10-The therapeutic uses of sodium or potassium iodide include the following Except:
A-Prophylaxis of endemic goiter.
B-Preoperative preparation before subtotal thyroidectomy.
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C-As antiseptic.
D-As expectorant.
11-Insulin release is augmented by the following Except:
A-Glucose.
B-Glucagon.
C-Vagal stimulation.
D-Alpha2 stimulation.
12-Actions of insulin do not include:
A-Facilitation of glucose transport into cells.
B-Facilitation of hepatic glycogenesis.
C-Facilitation of hepatic gluconeogenesis.
D-Inhibition of lipolysis in sdipose tissue.
13-The insulin receptor is:
A-Ion channel regulating receptor.
B-Tyrosine kinase linked receptor.
C-G-protein coupled receptor.
D-Cytoplasmic receptor.
14-The primary route of administration of insulin is:
A-Intradermal.
B-Subcutaneous.
C-Intravenous.
D-Intramuscular.
15-The duration of action of lente insulin is:
A- 2-4 hours.
B- 8-10 hours.
C- 20-24 hours.
D- 30-36 hours.
16-The most dangerous adverse reaction of insulin is:
A-Hypoglycemia.
B-Lipodystrophy.
C-Allergy.
D-Resistance.
17-There is no alternative to insulin therapy for:
A-All type I D.M. patients.
B-All type II D.M. patients.
C-Type II D.M. patients not controlled by sulphonylureas.
D- Type II D.M. patients not controlled by metformin biguanide.
18-The insulin preparation of choice in diabetic ketoacidosis (DKA):
A-Regular insulin.
B-Lente insulin.
C-Isophane insulin (N.P.H.).
D-Glargine insulin.
19-2nd generation sulphonylureas differ from 1st generation in that they are:
A-More potent.
B-Longer acting.
C-Do not cause hypoglycemia.
D-Do not release insulin from the pancreas.
20-Sulphonylureas do not lower blood glucose level in:
A-Non-diabetics.
B-Type I D.M.
C-Type II non-obese diabetic patients.
D-Type II obese diabetic patients.
21-Which of the following drugs can precipitate hypoglycemia in patients treated with sulphonylureas:
A-Phenytoin.
B-Rifampicin.
C-Prednisolone.
D-Chloramphenicol.
22-The hypoglycemic action of sulphonylureas is attenuated by the concurrent use of:
A-Hydrochlorothiazide.
B-Sulphonamides.
C-Aspirin.
D-Phenylbutazone.
23-Which of the following is not a sulphonylurea but acts by a similar mechanism of action and is preferred in patients allergic to sulphonamides:
A-Glimperide.
B-Miglitol.
C-Repaglinide.
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D-Rosiglitazone.
24-Long term therapy with metformin may lead to the following type of anemia:
A-Iron deficiency anemia.
B-Pernicious anemia.
C-Aplastic anemia.
D-Folic acid deficiency anemia.
25-Metformin is contraindicated in the following patients Except:
A-Patients with COPD.
B-Patients with congestive heart failure.
C-Patients with hepatocellular failure.
D-Obese type II D.M.
26-The Na+ retaining action of aldosterone is exerted on the:
A-Proximal convoluted tubule.
B-Cortical diluting segment.
C-Ascending limb of loop of Henle.
D-Distal convoluted tubule.
27-Hydrocortisone (cortisol) exerts the following action:
A-Increases both K+ and Ca2+ excretion.
B-Increases K+ and decreases Ca2+ excretion.
C-Decreases K+ and increases Ca2+ excretion.
D-Decreases both K+ and Ca2+ excretion.
28-Corticosteroids exert their anti-inflammatory action by inhibiting the following enzyme:
A-Cyclooxygenase.
B-Phosphodiesterase.
C-5-Lipooxygenase.
D-Phospholipase A2.
29-The glucocorticoid having mineralocorticoid activity is:
A-Triamcinolone.
B-Hydrocortisone.
C-Beclomethasone.
D-Dexamethasone.
30-Corticosteroids can aggravate the following diseases Except:
A-Congenital adrenal hyperplasia.
B-Hypertension.
C-Peptic ulcer.
D-Diabetes mellitus.
31-For management of cerebral edema due to brain tumors, betamethasone and dexamethasone are preferred because they:
A-Do not cause Na+ and water retention.
B-Are more potent.
C-Can treat brain tumors.
D-Can be given by injection.
32-Which of the following bones are affected more by glucocorticoid-induced osteoporosis:
A-Lumbar vertebrae (spine).
B-Femur.
C-Radius.
D-Hip bone.
33-The following adverse effect of glucocorticoids is due to glucocorticoid actions Except:
A-Moon face.
B-Peptic ulcer.
C-Hypertension.
D-Osteoporosis.
34-Which of the following is a 5-α-reductase inhibitor useful in benign prostatic hyperplasia and male pattern baldness:
A-Flutamide.
B-Finasteride.
C-Cyproterone.
D-Danazol.
35-Hormonal replacement therapy with estrogen in post-menopausal females increases the risk of the following disorders Except:
A-Gall stones.
B-Osteoporosis.
C-Endometrial carcinoma.
D-Thromboembolic diseases.
36-Estrogen therapy can worsen the following conditions Except:
A-Migraine.
B-Cholelithiasis.
C-Acne vulgaris.
D-Hypertension.
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37-In which of the following forms of oral contraception pills are taken continuously without interruption:
A-Combined pills.
B-Post-coital pills.
C-Minipills.
D-Triphasic pills.
38-Concurrent use of which of the following drugs is likely to cause failure of oral contraceptives:
A-Isoniazid.
B-Rifampicin.
C-Cimetidine.
D-Allopurinol.
39-The following drug can decrease vitamin D and cause osteomalacia if prescribed for long periods:
A-Tetracycline.
B-Ciprofloxacin.
C-Phenytoin.
D-Digoxin.
40-Biphosphonates are beneficial in the following conditions Except:
A-Paget's disease.
B-Senile osteoporosis.
C-Rickets.
D-Osteolytic bony metastasis.
Answers of MCQs:
1-C 2-A 3-C 4-A 5-B 6-D 7-A 8-B 9-D 10-C 11-D 12-C 13-B 14-B 15-C 16-A 17-A 18-A 19-A 20-B 21-D 22-A 23-C 24-B 25-D 26-D 27-A 28-D 29-B 30-A 31-A 32-A 33-C 34-B 35-B 36-C 37-C 38-B 39-C 40-C
Revision on Blood
Give an Account on:
1-Unfractionated heparin (UFH): mechanism of action-adverse effects –contraindications.
2-The advantages of low molecular weight heparins (LMWH) over unfractionated heparins (high molecular heparins).
3-Oral anticoagulants (warfarin –dicuomarol) as regards: mechanism of action- adverse effects – contraindications – drug interactions.
4-What is the mechanism of action of:
-Streptokinase (fibrinolytics = thrombolytics).
-Dipyridamole.
-Simvastatin.
-Cholestyramine.
5-Iron preparations and treatment of acute iron toxicity.
Compare between heparin and warfarin as regards: mechanism of action-pharmacokinetics- onset and duration of action - control of the dose-reversal of action.
Give Reason:
1-Heparin acts as an anticoagulant both in vivo and in vitro.
2-Warfarin acts only in vivo and not in vitro.
3-In prophylaxis against deep venous thrombosis both heparin and warfarin are co-administered at the start, then heparin is stopped and warfarin therapy is continued.
4-Alteplase (r-tPA) is preferred to streptokinase.
5-Folinic acid is not used alone in treatment of pernicious anemia.
Answer the following MCQ: )
1-Absorption of oral iron is facilitated by the following Except:
A-Antacids containing magnesium and / or alumunium salts.
B-Tetracyclines.
C-Phosphates.
D-Ascorbic acid.
2-Iron sorbitol citric acid differs from iron dextran in that:
A-It can not be injected IV.
B-It is not excreted in urine.
C-It is not bound to transferring in plasma.
D-It causes fewer adverse effects.
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3-Megaloblastic anemia occurs in:
A-Vitamin B12 but not folic acid deficiency.
B-Folic acid but not Vitamin B12 deficiency.
C-Either folic acid or Vitamin B12 deficiency.
D-Only combined Vitamin B12 and folic acid deficiency.
4-Megaloblastic anemia due to folate deficiency may occur by:
A-Phenytoin therapy.
B-Trimethoprim therapy.
C-Pyrimethamine or Proguanil therapy.
D-All of the above.
5-Vitamin K injection is indicated in treatment of bleeding occurring in patients:
A-Being treated with heparin.
B-Being treated with streptokinase.
C-Of obstructive jaundice.
D-Of peptic ulcer.
6-Heparin is contraindicated in the following conditions Except:
A-Pulmonary T.B.
B-Threatened abortion.
C-Subacute bacterial endocarditis.
D-Disseminated intravascular coagulopathy.
7-The following statement about oral anticoagulants is Incorrect:
A-They interfere with an early step in synthesis of coagulation factors
B-They have a latency of onset of about 3 days.
C-Their dose is adjusted by repeated measurement of prothrombin time and international normalized ratio (INR).
D-They are contraindicated in pregnancy and lactation.
8-When using warfarin in prophylaxis of deep venous thrombosis you attempt to make INR:
A- 1.3– 1.5
B- 1.5- 1.8
C- 2-3
D- 3-5
9-The following drug reduces the effect of warfarin:
A-Ampicillin.
B-Cimetidine.
C-Aspirin.
D-Estrogen (as oral contraceptive).
10-The following drug prolongs prothrombin time when given to a patient treated with oral anticoagulants:
A-Frusemide.
B-Rifampicin.
C-Vitamin K.
D-Oral contraceptives.
11-Which fibrinolytic selectively activates plasminogen bound to fibrin rather than circulating plasminogen:
A-Urokinase.
B-Streptokinase.
C-Alteplase (r-tPA).
D-None of the above.
12-The most important complication of streptokinase is:
A-Bleeding.
B-Hypotension.
C-Fever.
D-AV block.
13-A patient has an attack of hematemesis following streptokinase therapy, which of the following drugs is most effective in controlling this bleeding:
A-Vitamin K.
B-Aminocaproic acid.
C-Protamine sulphate.
D-Rutin.
14-Tranexamic acid is the specific antidote of:
A-Heparin.
B-Dicuomarol.
C-Iron.
D-Alteplase.
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15-Pediatric aspirin prolongs bleeding time by inhibiting synthesis of:
A-Coagulation factors in the liver.
B-Prostacyclin (PGI2) in vascular endothelium.
C-TXA2 in platelets.
D-c-AMP in platelets.
16-Which of the following drugs inhibit platelet aggregation by increasing platelet c-AMP:
A-Sulphinpyrazone.
B-Dipyridamole.
C-Aspirin.
D-Ticlopidine.
Match:
17-Blocks GPIIb / IIa platelet receptors. 18-Prevents ADP-dependent platelet aggregation. 19-Inhibits cholesterol synthesis by inhibition of HMG-CoA reductase enzyme. 20-Synthetic pentasaccharide used in prophylaxis of DVT during orthopedic leg surgery.
A-Simvastatin.
B-Abciximab.
C-Ticlopoidine.
D-Fondaparinux.
Answers to MCQ:
1-D 2-A 3-C 4-D 5-C 6-D 7-A 8-C 9-D 10-A 11-C 12-A 13-B 14-D 15-C 16-B 17-B 18-C 19-A 20-D
Revision on Chemotherapy
Narrow Spectrum Antibiotics:
1-Penicillins: benzyl-procaine-benzathine-phenoxymethyl penicillins:
Active mainly against Gram positive bacteria.
2-Aminoglycosides: Active mainly against Gram negative bacteria and some Gram positive bacteria as Staph. and Strept., inactive against Anerobes.
3-Old Fluoroquinolones as ofloxacin, norfloxacin, and ciprofloxacin: Active against Gram negative bacteria and Staph., inactive against Strept. pneumonia and anerobes.
4-Monobactam: Aztreonam, active only on Gram negative bacteria.
5-Vancomycin: active mainly on Gram positive.
6-Bacitracin: active on Gram positive bacteria.
7-Polymyxins: active against Gram negative bacteria especially Pseudomonas.
Broad Spectrum Antibiotics:
1-Penicillins: broad spectrum as Ampicillin-Amoxycillin-Ampicillin esters (Proampicillins = Ampicillin prodrugs) and extended spectrum penicillins = Anti-pseudomonal penicillins as azlocillin, mezlocillin, carbenicillin, ticarcillin, and piperacillin.
2-Cephalosporins.
3-Carbapenems as Imipenem.
4-Co-Trimoxazole.
5-New Fluoroquinolones as sparfloxacin, gatifloxacin, moxafloxacin, levofloxacin, and trovafloxacin: active on Gram negative, Gram positive including Strept. pneumonia, and anerobes.
6-Chloramphenicol.
7-Tetracyclines.
8-Rifampicin (active against T.B., Leprosy,Gram positive, Gram negative, and pox virus).
Bactericidal Antibiotics:
1-All β-Lactam antibiotics: Penicillins-Cephalosporins-Carbapenems-Monobactams.
2-Aminoglycosides ( bacteriostatic on T.B. bacilli).
3-Co-Trimoxazole.
4-Fluoroquinolones.
5-Vancomycin.
6-Bacitracin.
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7-Polymyxins: polypeptide antibiotic (ineffective orally)-acts on the cell membrane-active on Gram negative-used only locally and never systemically as they are extremely nephrotoxic. Active against Gram negative bacteria especially Pseudomonas. 7-Metronidazole. 8-Rifampicin.
Important Note:
Bactericidal antibiotics are divided into:
1-Concentration-Dependent Antibiotics: as Aminoglycosides and Fluoroquinolones. They have Post-Antibiotic Effect (PAE) i.e. persistent suppression of bacterial growth after limited exposure to antibiotics. 2-Time-Depenent Antibiotics: as β-Lactam antibiotics and Vancomycin
Bacteriostatic Antibiotics:
1-Sulphonamides. 2-Trimethoprim. 3-Chloramphenicol. 4-Tetracyclines. 5-Spectinomycin: related to aminoglycosides-used in treatment of gonorrhea in penicillin allergic patients-main adverse effect is nephrotoxicity.
Antibiotics acting as Bacteriostatic or Bactericidal:
1-Macrolides (erythromycin-clarithromycin-azithromycin)- Lincosamines (clindamycin- lincomycin) –and Ketolides (telithromycin): act as bacteriostatic drugs in low concentrations and as bactericidal drugs in high concentrations. 2-Isoniazid (anti-T.B.) is bacteriostatic on dormant sluggish bacilli and bactericidal on active bacilli.
Antibiotics active against anerobes:
1-Metronidazole. 2-Clindamycin. 3-Cephalosporins especially cefoxitin. 4-Penicillins. 5-Broad spectrum antibiotics: tetracyclines and chloamphenicol. 6-New Fluoroquinolones as sparfloxacin, gatifloxacin, moxafloxacin, levofloxacin, and trovafloxacin.
Antibiotics inactive against anerobes:
1-Aminoglycosides. 2-Old Fluoroquinolones as ofloxacin, norfloxacin, and ciprofloxacin.
Mechanism of Action of Antimicrobials:
I- Inhibitors of Cell Wall Synthesis:
1-β-Lactam antibiotics: Penicillins-Cephalosporins-Carbapenems (Imipenem, Meropenem, Ertapenem) –Monobactams (Aztreonam).
2-Vancomycin.
3-Cycloserine (2nd line anti-T.B., causes CNS toxicity).
4-Isoniazid (INH): 1st line anti-T.B. that inhibits mycolic acid synthesis.
II-Antibiotics Interfering with Cell Membrane:
1-Polymyxins.
2-Polyene Antifungal Antibiotics: Amphotericin B and Nystatin produce channels in the fungal cell membrane made of ergosterol leading to leakage of fungal cell contents as electrolytes.
3-Azoles: Antifungal antibiotics as Ketoconazole that inhibit ergosterol synthesis by inhibition of CYP450.
4-Terbenafine: Antifungal, inhibits ergosterol synthesis but does not inhibit CYP450.
III- Inhibitors of Protein Synthesis:
1-Binbing to 50 S ribosomal subunit: Macrolides-Lincosamines-Ketolides (inhibit translocation step) and Chloramphenicol (inhibit peptidyl transferase).
2-Binding to 30 S ribosomal subunit: Aminoglycosides (misreading of m-RNA and irreversible inhibition of protein synthesis), and Tetracyclines (inhibit t-RNA from reaching m-RNA-ribosome complex).
IV-Inhibitors of RNA synthesis:
Rifampicin: inhibits DNA-dependent RNA polymerase enzyme.
V- Inhibitors of DNA synthesis:
1-Quinolones and Fluoroquinolones: inhibit DNA gyrase (Topoisomerase II).
2-Antiviral Drugs as Acyclovir and Gancyclovir which inhibit DNA polymerase, and Zidovudine which inhibits reverse transcriptase (RNA-dependent DNA polymerase in HIV).
3-Antifungal Drugs as Flucytosine.
4-Antiamoebic Drugs as Metronidazole.
5-Antimalarial Drugs as Chloroquine.
6-Antibilharzial Drugs as Oxamniquine.
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VI-Inhibitors of Metabolic Pathway (Antimetabolites):
1-Sulphonamides: competitive inhibitors of dihydropteroate synthetase enzyme (by chemical similarity with PABA). 2-Trimethoprim. 3-Proguanil. 4-Pyrimethamine. They inhibit dihydrofolate reductase in bacteria and malaria and accordingly inhibit synthesis of active tetrahydrofolic acid. They may cause megaloblastic anemia. 5-Co-Trimoxazole: combination of sulpha (sulphamethoxazole) and trimethoprim leading to "sequential block". 6-Methotrexate: anticancer antimetabolite folic acid analogue that inhibits dihydrofolate reductase.
Antibiotics Mainly Excreted Unchanged in Urine:
1-Penicillins except Nafcillin. 2-Cephalosporins except Ceftriaxone and Cefoperazone (3rd generation). 3-Carbapenems. 4-Monobactams. 5-Aminoglycosides. 6-Vancomycin. 7-Tetracyclines except Doxycycline.
RULES:
1-They are effective in treatment of UTIs. 2-The dose should be adjusted in old age and in renal impairment according to "creatinine clearance". 3-The duration of action of penicillins and cephalosporins can be increased by adding probenicid because they are excreted by active tubular secretion (active transport).
Antibiotics Mainly Metabolised by The Liver:
1-Macrolides –Lincosamines-Ketolides.
2-Chloramphenicol.
RULES:
1-They are much less effective in treatment of UTIs.
2-The dose must be adjusted according to liver functions.
Antibiotics Partly Metabolized and Partly Excreted
Unchanged:
1-Fluoroquinolones.
2-Sulphonamides.
Antibiotics Excreted in Bile:
1-Nafcillin.
2-Ceftriaxone and Cefoperazone.
3-Doxycycline.
RULES:
1-They are long acting due to entero-hepatic circulation which allows once / day dose and this improves patient's compliance and reduces the liability of bacterial resistance.
2-They do not require dose adjustment in old age and renal impairment.
3-They are very effective in treatment of GIT infections as typhoid fever and bacillary dysentery, and in biliary tract infections.
Antibiotics Acting as HME Inducers:
1-Rifampicin.
2-Griseofulvin (antifungal in treatment of muco-cutaneous infections).
Antibiotics Acting as HME Inhibitors:
1-Macrolides except Azithromycin.
2-Fluoroquinolones.
3-Chloramphenicol.
4-Ketoconazole.
Antibiotics That Are Safe In Pregnancy, Lactation, and Newborn:
1-β-Lactam antibiotics as Penicillins and Cephalosporins.
2-Macrolides.
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Antibiotics That Are Unsafe In Pregnancy, Lactation, and Children: 1-Aminoglycosides: may cause fetal deafness if used in pregnancy. 2-Vancomycin (as aminoglycosides). 3-Fluoroquinolones: may cause arthropathy and affect bone growth if given in pregnancy, lactation, and pre-pubertal children. 4-Chloramphenicol: Gray baby syndrome. 5-Tetracyclines are teratogenic and precipitate in bone and teeth (chelate with Ca2+) and cause deformity. 6-Sulphonamides: may cause hyperbilirubinemia and kernicterus by displacing bilirubin from plasma proteins.
Antibiotics That Should Never Be Used Systemically:
1-Neomycin: used orally, topically on the skin, and by inhalation. Never given systemically to avoid nephrotoxicity and ototoxicity. 2-Bacitracin: polypeptide antibiotic-inhibits cell wall synthesis-active on Gram positive as Staph.aureus-used only on skin-extremely nephrotoxic. 3-Polymyxins (see before). 4-Nystatin: antifungal –polyene- drug of choice in treatment of moniliasis-given orally ant topically on skin and vagina-extremely nephrotoxic if used systemically. 5-Topical Azoles: Miconazole-Clotrimazole-Econazole; antifungal drugs. 6-Idoxuridine: antiviral against herpes simplex virus-used in treatment of viral keratitis.
Topical Antibiotics:
1 to 6 : see before. 7-Erythromycin: in treatment of skin infections and acne vulgaris. 8-Gentamicin: in treatment of skin infections and catheter sterilization. 9-Chloramphenicol: in eye and ear infections. 10-Tetracyclines: in skin and eye infections. 11-Topical Sulphonamides: Sulphacetamide eye drops – Silver Sulphadiazine in burn and skin infections- Mafenide in skin and wound infections. 12-Ketoconazole: used topically as hair shampoo in treatment of hair dandruff.
Antibiotics Used in Proststitis:
1-Trimethoprim.
2-Co-trimoxazole.
3-Fluoroquinolones.
Nephrotoxic Antibiotics:
1-Aminoglycosides (especially if given with loop diuretics and cephalosporins).
2-Vancomycin.
3-Cephalosporins.
4-Methicillin (anti-staph. penicillin, it is obsolete due to high incidence of acute interstitial nephritis).
5-Imipenem used alone (without dihydropeptidase inhibitors as cilastatin).
6-Tetracyclines: may induce nephrogenic diabetes insipidus especially demeclocycline. Expired tetracyclines (=outdated) cause Fanconi's syndrome.
7-Sulphonamides: acetylated in the liver into insoluble metabolite causing crystalluria (prevented by proper hydration and NaHCO3).
8-Amphotericin B.
Hepatotoxic Antibiotics:
1-Sulphonamides.
2-Tetracyclines.
3-Trovafloxacin (new Fluoroquinolone).
4-Ketoconazole.
Antibiotics Causing Cholestatic Hepatitis and Jaundice
1-Erythromycin (due to estolate ester).
2-Rifampicin.
Antibiotics Causing Ototoxicity:
1-Aminoglycosides.
2-Vancomycin.
Antibiotics Causing Bone Marrow Depression:
1-Chloramphenicol.
2-Sulphonamides.
3-Co-Trimoxazole.
4-Amphotericin B.
5-Zidovudine.
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Antibiotics Causing Seizures (Convulsions):
1-Penicillins especially in large doses and by intrathecal injection. 2-Carbapenems as imipenem. 3-Fluoroquinolones especially with NSAIDs as aspirin or with theophylline. 4-Cycloserine.
Causes of Bleeding by Antibiotics:
1-Killing of bacterial flora that synthesize vitamin K in gut by broad spectrum antibiotics especially if incompletely absorbed as tetracyclines and ampicillin. 2-Anti-vitamin K action in the liver as cephalosporins. 3-Platelet dysfunction by carbenicillin and ticarcillin (extended spectrum penicillins) and moxalactam (3rd generation cephalosporins). 4-Displacement of oral anticoagulants as warfarin from plasma proteins by sulphonamides.
Causes of Bacterial Resistance:
A-Natural Resistance: Mycoplasma are resistant to β-lactam antibiotics due to absence of peptidoglycan cell wall.
B-Acquired (plasmid-mediated):
1-Synthesis of enzymes causing destruction of the drug, as β-lactamases produced by bacteria as Staph. aureus and Pseudomonas. 2-Alteration of the binding site of the antibiotic. 3-Decrease permeability of bacterial cell to antibiotics. 4-Increased synthesis of PABA antagonizes sulphonamides.
Answer The Following Questions:
1-Give an account on the following chemotherapeutics as regards mechanism of action, therapeutic uses, and adverse effects: -Ampicillin (Penicillins). -Amoxycillin. -Ofloxacin (Fluoroquinolones). -Co-trimoxazole. -Gentamicin (Aminoglycosides). -Vancomycin. -Metronidazole.
2-Discuss Cephalosporins as regards: mechanism of action, classification, and adverse effects.
3-Classify Anti-tuberculous drugs, discuss the mechanism of action and toxicity of rifampicin and isoniazid.
4-Give an account on Anti-bilharzial drugs.
5-Mention Penicillins used in treatment of infections caused by β-lactamase producing bacteria.
Answer:
(A-β-Lactamase resistant penicillins as cloxacillin, dicloxacillin,…
B-Adding β-lactamase inhibitors as clavulanic acid, sulbactam, and tazobactam to broad spectrum or extended spectrum penicillins).
6-Indicate True, False, or I don't know and mention why:
A-Cephalosporins can replace penicillins in treatment of staph. infections in non-allergic patients.
B-3rd and 4th generation cephalosporins can be safely used in treatment of staph. infections in penicillin-allergic patients.
C-Penicillins are among the safest antibiotics in non-allergic patients.
D-Aminoglycosides are highly effective against anerobic bacteria.
E-Aminoglycosides are better avoided in patients with myasthenia gravis.
F-The dose of theophylline should be increased in patients treated with erythromycin.
G-Chloramphenicol and aminoglycosides are considered as a favorable antimicrobial combination.
H-The dose of doxycycline should be carefully adjusted in patients with renal impairment.
I-Co-trimoxazole is preferred to sulphonamides as antimicrobial.
J-Trimethoprim may induce pernicious anemia on prolonged use.
7-Give Reason (Explain on pharmacological basis):
A-Penicillins are combined to aminoglycosides in treatment of serious infections, however they should not mixed in the same syringe or infusion fluid.
B-Erythromycin is used in treatment of diabetic gastroparesis.
C-Penicillins are among the safest antibiotics provided there is no allergy.
D-Imipenem should be combined to cilastatin in treatment of serious infections.
E-Proampicillins as bacampicillin are preferred to ampicillin.
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F-Patients treated with sulphonamides should be properly hydrated
and use NaHCO3.
G-Pyridoxine (vitamin B6) should be prescribed prophylactically in
tuberculous patients treated by INH.
8-Comment on the following combinations, whether favorable or
unfavorable with explanation:
A-Sulphamethoxazole + Trimethoprim.
B-Ampicillin + Tetracycline.
C-Amoxycillin + Clavulanic acid.
D-Cefradine + Probenicid.
E-Imipenem + Cilastatin.
F-Ticarcillin + Sulbactam.
G-Ofloxacin + NSAIDs.
H-Rifampicin + INH.
I-Gentamicin + Frusemide.
J-Streptomycin + competitive NMBs as curare.
K-Ciprofloxacin + Aluminium- containing antacids.
L-Amphotericin B + Ketoconazole.
M-Tetracyclines + Sucralfate.
N-Tetracycline + ferrous fumarate.
O-Ketoconazole + Famotidine.
9-A 56 year old patient with prosthetic valve was about to undergo a
dental procedure and the dentist decided to give him procaine
penicillin 300.000 Units IM for prophylaxis against endocarditis.
Unfortunately he developed anaphylactic shock.
A-What is the cause of shock in this patient?
B-How could anaphylactic shock be avoided?
C- ---------- is a life saving drug in this type of shock and is given by --
--injection. ----------- and ---------- are also useful in this case.
D-In the future all the following antibiotics can be used in this patient
to guard against enocarditis except:
i-Vancomycin.
ii-Cefazolin.
iii-Sulphonamides.
iv-Erythromycin.
v-Aminoglycosides.
10-A 43 year old diabetic female suffers from monilial vulvo-vaginitis:
A-The drug of choice is:
i-Nystatin.
ii-Metronidazole.
iii-Chloramphenicol.
iv-Acyclovir.
v-Praziquantel.
B-The mechanism of action of the selected drug is:
i-Inhibition of cell wall synthesis.
ii-Inhibition of fungal DNA synthesis.
iii-Interference with cell membrane forming channels.
iv-Interference with folic acid synthesis.
v-Inhibition of protein synthesis.
C-The route of administration in this patient is:
i-Oral.
ii-I.V.
iii-Topical.
iv-Intrathecal.
v-S.C.
D-The dug selected in A is chemically:
i-Azole.
ii-Macrolide.
iii-Quinolone.
iv-Polyene.
v-Aminoquinoline.
11-A 17 year old female is having a problem with acne vulgaris, and her physician decided to use oral antibiotic. Several weeks later she developed severe diarrhea that was diagnosed as "pseudomembranous colitis due to superinfection with Clostridium difficile".
A-Most probably the oral antibiotic used to treat acne in this patient is:
i-Vancomycin.
ii-Doxycyline.
iii-Clindamycin.
iv-Erythromycin.
v-Amphotericin.
B-What is the mechanism of action of the drug selected in the previous question?
C-How to treat pseudomembranous colitis in this case?
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12-A 29 year old Egyptian farmer was diagnosed as having mixed infection with S.hematobium and S.mansoni.
A-What is the drug of choice for this patient?
B-What is the mechanism of action of the selected drug?
C-What are the advantages of this drug?
D-What are the adverse effects of this drug?
-Matching: 13-Drug of choice in Pneumocystis carinii. A-Rifampicin. 14-Long acting penicillin used in B-Doxycycline. prophylaxis against streptococcal infections in patients with RF. 15-4th Generation cephalosporin. . C-Vancomycin. 16-Arthropathy and abnormal bone growth. D-Co-trimoxazole 17-Used only topically to avoid systemic toxicity. E-Aztreonam. 18-Red-man syndrome is a characteristic adverse F-Benzathine effect if given rapidly IV. Penicillin. 19-A new tetracycline that does not require G-Neomycin. dose adjustment in renal impairment. 20-Maculopapular rash if administered H-Sulphonamide. to patients with infective mononucleosis. 21-Flu-like syndrome occurs at beginning I-Ampicillin. of treatment.
22-Kernicterus is a serious adverse effect. J-Cefipime.
K-Ciprofloxacin.
ANSWERS:
Question 6-
A: True. Cephalosporins are resistant to β-lactamases especially 3rd and 4th generations. However they are better avoided in penicillin-allergic patients because 10% of population show cross allergy with cephalosporins due to structural similarity.
B-False: see before.
C-True: penicillins have "selective toxicity" because they inhibit cell wall synthesis which is present in bacteria and not in humans.
D-False: Aminoglycosides are ineffective against anerobes because they need oxygen-dependent active transport to enter inside bacterial cells and inhibit protein synthesis.
E-True: Aminoglycosides inhibit releases of acetylcholine from motor nerves and may have a blocking effect on Nm receptors in NMJ thus causing skeletal muscle weakness.
F-False: Erythromycin is a HME inhibitor (inhibits CYP450) so it reduces metabolism (clearance) of theophylline, and accordingly we should reduce the dose of theophylline in patients receiving erythromycin.
G-False: Aminoglycosides are bactericidal antibiotics which act on active growing and multiplying bacteria, whereas chloramphenicol is a bacteriostatic drug which inhibits bacterial growth and multiplication and accordingly antagonizes the cidal effect of aminoglycosides.
H-False: Doxycycline is mainly eliminated by biliary excretion and not by renal excretion, so it does not require dose adjustment in patients with renal impairment.
I-True: it is a combination of sulphamethoxazole and trimethoprim with the following advantages: synergistic action of both drugs – broader spectrum – less toxicity – less liable to cause bacterial resistance – more effective in treatment of mixed infections – effective in pneumocystis carinii- effective in prostatitis.
J-False: Trimethoprim may cause megaloblastic anemia due to reduced synthesis of folinic acid but does not affect B12.
Question 7-:
A- Penicillins and aminoglycosides are synergistic because both are bactericidal drugs acting by different mechanisms. However, they should not be mixed in the same syringe as they chemically antagonize each other as penicillins are acidic compounds whereas aminoglycosides are basic compounds.
B- Erythromycin –in addition to its antibacterial action- has a prokinetic action, i.e. it increases gastric motility and stimulates gastric emptying by stimulation of motilin receptors.
C- see question 6-C.
D- Imipenem is not used alone in treatment of infection because it is metabolized by dihydropeptidase in renal cells into an inactive nephrotoxic metabolite, so it should be combined with cilastatin which is a dihydropeptidase inhibitor (imipenem + cilastatin = tienam).
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E- Ampicillin is incompletely absorbed orally especially in the presence of food and this causes diarrhea and superinfection but proampicillins are completely absorbed then de-esterified in gut mucosa and liver into ampicillin, they cause minimal gut upset and achieve higher blood levels. F- Sulphonamides are metabolized in the liver by acetylation and the acetylated metabolite is then excreted in urine. It is insoluble in acidic urine and may cause crystalluria, renal colics, hematuria and even anuria due to renal damage. This is avoided by proper hydration and using NaHCO3 to render the urine alkaline. G- Isoniazid competes with pyridoxine (B6) due to structural similarity and interferes with myelination of nerves especially in slow acetylators, that is why B6 should be given to prevent peripheral neuritis.
Question 8:
A- Favorable combination (see question 6-I).
B- Unfavorable combination: Ampicillin is a bactericidal drug but Tetracyclines are bacteriostatic drugs and thus antagonize the action of ampicillin. C- Favorable combination: Amoxycillin is a broad spectrum penicillin but is β-lactamase sensitive and is ineffective against staph. infections, so clavulanic acid is added to act as β-lactamase inhibitor to protect amoxicillin (amoxycillin + clavulanic acid = augmentin). D- Favorable combination: Cefradine as most cephalosporins is excreted in urine by active transport which can be reduced by adding probenicid thus leading to prolongation of action of cefradine.
E- Favorable combination: see question 7-D.
F- Favorable combination: Ticarcillin is an extended- spectrum penicillin (anti-pseudomonal penicillin) but is β-lactamase sensitive so combining it with sulbactam which is a β-lactamase inhibitor protects ticarcillin against β-lactamase and renders it active against β-lactamase producing bacteria as staph. G- Unfavorable combination: Ofloxacin (a fluoroquinolone) is better avoided with NSAIDs to avoid the possibility of inducing seizures (convulsions). H- Favorable combination: Rifampicin and INH is the most important combination therapy in treatment of T.B.: they delay the occurrence of bacterial resistance-achieve synergism-less toxicity. I- Unfavorable combination: both gentamicin (aminoglycoside antibiotic) and frusemide (loop diuretic) are ototoxic drugs and such combination may cause permanent damage of the 8th cranial nerve leading to irreversible deafness and vertigo.
J- Unfavorable combination: streptomycin causes skeletal muscle relaxation and weakness by inhibition of release of acetylcholine from somatic nerves and having curare-like action on Nm receptors in NMJ, this will be exaggerated if competitive NMBs are used in the same patient.
K- Unfavorable combination: Al-containing antacids reduce oral absorption and oral bioavailability of many drugs including fluoroquinolones as ciprofloxacin (also decrease absorption of tetracyclines, digoxin, ketoconazole, and phenytoin).
L- Unfavorable combination: Azoles as Ketoconazole will antagonize the action of Amphotericin B which is a polyene antifungal antibiotic that acts by forming channels in the fungal cell membrane leading to leakage of cell contents and fungal cell death whereas Ketoconazole inhibits synthesis of ergosterol thus inhibiting fungal cell membrane synthesis.
M- Unfavorable combination if administered orally at the same time because sucralfate (is a mucosal protective agent used in treatment of P.U. and prevents recurrence) contains aluminium which reduces absorption of tetracyclines.
N-Unfavorable combination if given together as chelation occurs and this decreases oral absorption of both tetracyclines and oral iron preparations as ferrous fumarate used in treatment of iron deficiency anemia.
O- Unfavorable combination if given together as famotidine (H2 antagonist) markedly reduces gastric acidity which is essential for absorption of ketoconazole.
Question 9:
A- The patient is allergic to penicillin and antigen (penicilloic acid acts as a hapten) –antibody reaction occurred with release of histamine which resulted in severe V.D., hypotension, and bronchospasm (characteristics of anaphylactic shock).
B- Anaphylactic shock could be avoided by asking the patient about past history of penicillin administration and by intradermal (skin) test.
C- Adrenaline-IM-Corticosteroids as hydrocortisone IV-Antihistaminics as chlorpheniramine or fexofenadine.
D- ii: Cefazolin should be avoided in this patient as there is cross allergy between penicillins and cephalosporins in 10% of people due to similarity in chemical structure (both contain β-lactam ring).
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Question 10:
A- i:Nystatin.
B- iii.
C- iii.
D- iv.
Question 11:
A- iii: Clindamycin.
B- inhibition of bacterial protein synthesis by binding to 50 S ribosomal subunit (same mechanism as macrolide antibiotics).
C- Oral vancomycin and metronidazole.
Question 12:
A- Praziquantel.
B-Increases Ca2+ influx into bilharzial worm leading to spastic paralysis and death.
C-Advantages:
1-Easily administered orally. 2-Single oral dose. 3-Excellent compliance. 4-Treats both S. hematobium and mansoni. 5-Well tolerated due to mild adverse effects.
D-Adverse effects:
1-anorexia, nausea, abdominal pain, diarrhea. 2-Headache and dizziness. 2-fever, arthralgia, myalgia, and pruritus due to release of dead worm contents. 13-D 17-G 14-F 18-C 21-A 15-J 19-B 22-H 16-K 20-I
Answer the following questions:
I- Ennumerate 6 therapeutic uses of muscarinic agonists giving at least one example of the drugs used. (6 marks)
II- Explain (give reason): (1 mark each)
1- Acetylcholine has no therapeutic uses.
2- Carbachol causes twitches of the eye lids when applied locally in the eye but pilocarpine does not.
3- Neostigmine and not physostigmine is used in treatment of myasthenia gravis.
4- Edrophonium is used in diagnosis and not in treatment of myasthenia gravis.
III- Give an account on :
1- Manifestations and treatment of acute organophosphorous toxicity. (4 marks)
2- Differentiation between "myasthenic crisis" and "cholinergic crisis". (2 marks)
IV- Comment by "true", "false",or "I don't know" on the following statements: (1 mark each)
1- Synthetic choline esters are given by IV or IM injection.
2- Cholinesterase reactivators (Oximes) should be given as early as possible in treatment of organophosphorous toxicity.
3- The main fate of acetylcholine is through neuronal reuptake.
4- Carbachol is used in treatment of post-operative obstructive urine retention.
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Answer the following questions: (2)
1-Ennumerate 6 therapeutic uses of atropine and explain the pharmacological basis of each use. (6 marks) 2-Classify synthetic atropine substitutes, giving 2 examples in each group. (5 marks) 3-Give reason: (4 marks) a- Atropine should be given before neostigmine in diagnosis of myasthenia gravis. b- Hyoscine is contraindicated in old patients. c- Ipratropium is preferred to atropine in prophylaxis of bronchial asthma. d- Acidification of urine enhances urinary excretion of atropine. 4-Discuss briefly the manifestations and treatment of acute atropine toxicity. (6 marks) 5- Comment on the following statements by True or False: (4 marks) a- Atropine is commonly used for fundus examination. b- Hyoscine is the drug of choice in prophylaxis of motion sickness. c- Atropine is preferred to hyoscine as a pre-anaesthetic medication in thyrotoxic patients. 6- Complete: (9 marks) a- --------- and-------- are selective M1-blockers used in treatment of -------------- b- Tolterodine is a selective ------- blocker used in treatment of ------- c- Atropine is contraindicated in ------------- and ------------ d- ------------- and ----------- are antisecretory –antispasmodic atropine substitutes used in treatment of ------------ and ------------ e- The skin of a patient suffering from acute atropine toxicity is -------, ------------, and ---------- f- Tropicamide applied locally in the eye causes ---------, ----------,------and ---------
What is the Role of ----- in ----- :
Autonomic Nervous System:
1-Adrenaline (epinephrine) in anaphylactic shock.
2-Adrenaline in cardiac arrest.
3-Dopamine in shock (hypovolemic-cardiogenic).
4-Dobutamine in cardiogenic shock.
5-Salbutamol in bronchial asthma.
6-Phenylephrine in paroxysmal atrial tachycardia (PAT).
7-Fenoldopam in emergency hypertension.
8-Prazosin in hypertension.
9-Tamsulosin in benign prostatic hyperplasia.
10-Phenoxybenzamine in secondary hypertension due to pheochromocytoma.
11-Phentolamine in peripheral vascular diseases.
12-Beta blockers in hypertension.
13-Beta blockers in stable angina.
14-Propranolol in hyperthyroidism.
15-Beta blockers in congestive heart failure.
16-Labetalol in pheochromocytoma.
17-Carbachol in glaucoma.
18-Bethanechol in postoperative paralytic ileus and postoperative urine retention (non-obstructive).
19-Edrophonium in myasthenia gravis.
20-Neostigmine in myasthenia gravis.
21-Atropine in organophosphorous poisoning.
22-Hyoscine (scopolamine) in motion sickness.
Autacoids:
23-Ergotamine in migraine headache.
24-Sumatriptan in migraine headache.
25-Diphenhydramine in Parkinsonism.
26-Ondansetron in treatment of nausea and vomiting (antiemetic).
27-Aspirin in prevention of platelet aggregation.
28-Misoprostol in peptic ulcer.
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Respiration:
29-Methylxanthines in bronchial asthma. 30-Zileuton in bronchial asthma. 31-Montelukast in bronchial asthma. 32-Steroids in bronchial asthma. 33-Disodium cromoglycate in bronchial asthma. 34-Benzonatate in dry cough.
Diuretics:
35-Thiazide diuretics (hydrochlorothiazide) in hypertension. 36-Thiazide diuretics in nephrogenic diadetes insipidus. 37-Thiazide diuretics in idiopathic hypercalciuria. 38-Loop diuretics as frusemide in hypertension with renal impairment.
39-K+ sparing diuretics in edema. 40- K+ sparing diuretics in hypertension.
CVS:
41-Nitrates in stable angina. 42-Nitrates in Prinzmetal angina. 43-Beta blockers in stable angina. 44-Verapamil in stable angina. 45-Low-dose aspirin in stable angina. 46-Alpha methyl dopa in hypertension. 47-Clonidine in hypertension. 48-Prazosin in hypertension. 49-ACE inhibitors (Captopril) in hypertension. 50-AT1 receptor antagonists (Losartan) in hypertension. 51-Minoxidil in hypertension. 52-Hydralazine in hypertension. 53-Diazoxide in hypertension. 54-Sodium nitroprusside in hypertension. 55-Nifedipine in hypertension. 56-Digitalis in congestive heart failure. 57-Digitalis in atrial flutter or atrial fibrillation. 58-Bipyridines (Enamrinone-Milrinone) in heart failure.
CNS:
59-Morphine in acute pulmonary edema due acute left ventricular failure.
60-Morphine in renal or biliary colics.
61-Morphine in preanaesthetic medication.
62-Meperidine in obstetric analgesia.
63-Aspirin in inflammatory conditions.
64-Aspirin in fever.
65-Aspirin in chronic gout.
66-Indomethacin in patent ductus arteriosus.
67-Colchicine in gout.
68-Allopurinol in gout.
69-Rasburicase in gout.
70-Probenicid in gout.
71-L-dopa in Parkinsonism.
72-Bromocriptine in Parkinsonism.
73-Amantadine in Parkinsonism.
74-Deprenyl (Selegiline) in Parkinsonism.
75-Carbidopa and Benserazide in Parkinsonism.
76-Tolcapone and Entacapone in Parkinsonism.
77-Phenytoin in epilepsy.
78-Carbamazepine in epilepsy.
79-Ethosuccimide in epilepsy.
80-Valproic acid in epilepsy.
81-Barbiturates as phenobarbitone in epilepsy.
82 -Benzodiazepines as diazepam and clonazepam in epilepsy.
Enocrine:
83-Thioamides in hyperthyroidism.
84-Iodide in hyperthyroidism.
85-Radiactive iodine I131 in hyperthyroidism.
86-Insulin in IDDM.
87-Insulin in NIDDM.
88-Sulphonylyreas in NIDDM.
89-Metformin in NIDDM.
90-Meglitinides in NIDDM.
91-Thiazolidinediones in NIDDM.
92-Acarbose (or Miglitol) in D.M.
93-Raloxifen in postmenopausal females.
94-Finasteride in BPH.
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Chemotherapy:
95-Clavulanic acid in Staph. infections. 96-Cilastatin in serious bacterial infections. 97-Erythromycin in diabetic gastroparesis. 98-Praziquantel in Bilharziasis.
GIT:
99-Loperamide or Diphenoxylate in diarrhea. 100-Proton pump inhibitors in peptic ulcer. 101-H2-Antagonists in peptic ulcer. 102-Colloidal bismuth compounds in peptic ulcer. 103-Sucralfate in peptic ulcer. 104-Clarithromycin, Ampicillin, or Metronidazole in peptic ulcer. 105-Lactulose in hepatic insufficiency. 106-NaHCO3 in peptic ulcer.
Blood:
107-Simvastatin (Statins) in hyperlipidemia. 108-Fibrinolytics (Thrombolytics) as streptokinase in acute myocardial infarction. 109-Vitamin K in hypoprothrombinemia. 110-Protamine sulphate in heparin-induced hemorrhage.
Very Important:
In answering this type of questions we have to mention the mechanism of action of the required drug and the action related to the condition or disease, for example: *What is the role of corticosteroids in bronchial asthma?
Answer:
●Corticosteroids have anti-inflammatory action by inhibition of phospholipase A2 and accordingly inhibit synthesis of inflammatory mediators most importantly leukotrienes. ●They have antiallergic and immunosuppressive action by inhibiting antigen-antibody reaction and antibody synthesis. ●They increase the number of β2-receptors in bronchi and avoid tolerance to β2-agonists. ●They are not bronchodilators and so are not effective in acute attacks but are useful in prophylaxis of moderate intermittent asthma and are given by inhalation. Oral steroids are used in severe persistent asthma whereas hydrocortisone sodium succinate is the drug of choice in severe acute asthma (status asthmaticus). (If the answer is short we can give a brief account on the adverse effects or the disadvantages of the drug and its advantages as in "the role of NaHCO3 in peptic ulcer").
Final Pharmacology Exam 2008
PAPER (1) 04.06.2008:
Total Marks: 80 Marks divided as follows:
1-Essay Questions: 6 questions x 5 marks each = 30 marks:
Give an Account on:
☻Therapeutic uses of --------
☻Adverse (side) effects of --------
☻Contraindications of --------
☻Explain the role of ------- in --------
(Example: role of corticosteroids in bronchial asthma).
2-Give Reason: 5 questions x 2 marks each = 10 marks.
3- Compare: 5 questions x 4 marks each = 20 marks.
(Points of Similarity and Difference between 2 Drugs).
4-Mechanism of action:5 question x 2 marks each =10 marks
5-Drug Interactions: 5 questions x 2 marks each = 10 marks.
Comment whether the given drug combination is favorable or unfavorable and explain why.
(Examples: nitrates + hydralazine in angina is unfavorable= not recommended as they cause reflex tachycardia – alpha + beta blockers in treatment of pheochromocytoma is favorable= recommended to treat hypertension and cardiac arrhythmias).
PAPER (2) 05.06.2008:
Total Marks: 70 Marks divided as follows:
1-MCQs: 60 questions x half a mark each = 30 marks (only one answer is required in each question).
2-Mark (Mention) True or False and Explain Why:
20 questions x 1 mark each = 20 marks.
half a mark for true or false and half a mark for explanation
3-Complete (Fill in the blanks):
20 blanks x half a mark each = 10 marks.
4-Matching: 20 questions x half a mark each = 10 marks.
Pharmacology 3rd Year 2009
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Dr.Ahmed Abd El-Rahman www.medadteam.org
More than your dream
Subjects studied for both Essay and MCQ:
1-Autonomic Nervous System.
2-Cardiovascular System: Angina- Hypertension-
Heart Failure-Classification and mechanism of action of Anti-arrhythmics. 3-Kidney (Renal pharmacology = Diuretics + antidiuretics). 4-CNS + Treatment of Gout + DMARDs. 5-Endocrine pharmacology (Hormones). 6-Antibacterial Chemotherapy + Anti-Tuberculous drugs + Metronidazole. 7-GIT pharmacology. 8-Pharmacology of Respiration. 9-Pharmacology of Blood. 10-Autacoids. 11-Drug Interactions.
Subjects studied for MCQ only:
1-General Pharmacology. 2-Pharmacology of the Eye. 3-Skeletal muscle relaxants. 4-Anaesthesia: General and Local Anaesthesia. 5-Anti-Viral, Anti-Fungal, Anti-Malarial, Anti-Amebic, Anti-Bilharzial and other Anthelmintics. 6-Miscellaneous Subjects: Vitamins-Chelating Agents-Anabolic Steroids (steroids for body building)-Addiction-Immunopharmacology.
Make Your Answers "Clear and Precise"
G☺☺d Luck
Pharmacology Examination (4-6-2008)
1-Write a short account on the following (30 marks):
1-Mechanism of ACEIs in controlling heart failure.
2-Anitimicrobials used in treatment of Typhoid fever. Describe the mechanism of antimicrobial action of selected drugs.
3- Composition of Tiphasic hormonal contraceptive combination pills. List contraindictions of hormonal contraceptives.
4-Enumerate drugs used in grand mal epilepsy, their mechanism of action then mention side effects of one drug.
5- Classify antiemetic drugs according to their mechanism of action with examples.
6-Treatment of pernicious anemia describe their role in contolling this condition.
2-Give Reason (10 marks):
1-Certain drugs need gradual withdrawal after their prolonged use, give 4 examples.
2-Methadone is used in treating morphine addicts.
3- Oral anticoagulant drugs should be stopped 3- 4 days before operations.
4- Furosemide is preferred than thiazide diuretics in some clinical situations.
5- It is highly recommended to evaluate both renal and hepatic functions for the proper selection of cardiac glycosides for treating patients with heart failure.
3-Compare (20 marks):
1- Montelukast and salbutamol regarding their mechanism of action and role in bronchial asthma.
2- Nifedipine and verapamil: cardiovascular effects and uses, main side effects.
3- Morphine and butorphanol: the receptors affected and clinical importance.
4- Allopurinol and colchicine: mechanism of action and indications.
5- Buspirone and clonazepam: mechanism of action, advantages, and side effects.
4-The following enzymes are common drug targets. Select only one drug acting on it and mention its main therapeutic indication (10 marks).
1-COX lll.
2- Thromboxane A2 synthetase.
3- Phospholipase A2.
4- (HMG-CoA) reductase.
5- Lipooxygenase.
5- Evaluate the following drug combinations then comment on their interaction whether favourable or unfavourable then explain why (10 marks):
1- Oral anticoagulants with broad spectrum antibiotics.
2- Captopril combination to spironolactone.
3- Lithium combination to thiazide diuretics.
4- Propranolol combination to sulphonylureas.
5- Sulphamethoxazole combination to trimethoprim.
Best Of Luck
Pharmacology 3rd Year 2009
www.medadteam.org
41
Dr.Ahmed Abd El-Rahman www.medadteam.org
More than your dream
Pharmacology Exam (1)
Answer the following questions
1-Ennumerate 6 therapeutic uses of muscarinic agonists mentioning 2 examples of the drugs used. (6 marks)
2-Give an account on acute organophosphorous toxicity as regards: causes, manifestations, and treatment. (6 marks) 3-Give a brief account on "myasthenia gravis" as regards diagnosis, treatment, and differences between myasthenic and cholinergic crises. (5 marks) 4-Enumerate 6 therapeutic uses of atropine, and mention 1 atropine substitute for each use (if available). (6 marks)
5-Give an account on "acute atropine toxicity".
6-Classify synthetic atropine substitutes, mention at least 2 examples for each group. (7 marks)
7-Compare between atropine and hyoscine as regards: local actions- CNS actions. (4 marks)
8-Mention briefly the adverse effects of atropine. (4 marks)
9-What are the contraindications of atropine? (4 marks) 10-Give reason: (1 mark each) A-Atropine should be given before neostigmine in diagnosis of myasthenia gravis. B-Atropine may cause initial transient bradycardia if injected I.V. C-Large and toxic doses of atropine cause "atropine flush". D-Hyoscine is preferred to atropine as "pre-anaesthetic medication". E-Rabbits are tolerant to atropine. F-Ipratropium has replaced atropine in prophylaxis against bronchial asthma. G-Tropicamide is used instead of atropine in "fundus examination". 11-Complete: (1/2 mark for each blank) A-Atropine, hyoscine, and atropine substitutes are absolutely contraindicated in ------- and -------. B- -------- and ------- are atropine substitutes used in prophylaxis of bronchial asthma. C- --------- is the drug of choice in prophylaxis of motion sickness. D-Pirenzepine and telenzepine are selective ----- antagonists used in treatment of ---------. E-Synthetic antiparkinsonian atropine substitutes include ------ and -----. F- ------- is a selective M3 antagonist used in treatment of ---------. G-Benzhexol is a synthetic atropine substitute used in--------.
Answer the following questions:
1-Compare between heparin and warfarin as regards:
Mechanism of anticoagulant action- onset and duration of action- specific
antidote-control of dose.
2-Mention 4 drugs that increase the anticoagulant action of warfarin and
4 drugs that antagonize its anticoagulant action, explain why.
3-What are the advantages of LMWH over UFH?
4-Give a brief account on the mechanism of action and the role of
selective beta2 agonists in bronchial asthma.
5-Comment: some anti-inflammatory drugs are useful in bronchial
asthma therapy, but others are contraindicated.
6-Compare between thiazide diuretics and loop diuretics as regards:
Site of action- potency- effect on renal blood flow- indications.
7-Mention 4 drug interactions of loop diuretics.