Материал: MasterPass _ Pharmacology in 7 Days for Medical Students
Structure |
Parasympathetic effect |
Receptor involved |
Sympathetic effect |
Receptor |
|
|
|
|
involved |
|
|
|
|
|
Pregnant uterus |
Variable |
Ð |
Contraction (when pregnant |
α1 |
|
|
|
ladies get tense, they start |
|
|
|
|
having birth pains) |
|
Non-pregnant uterus |
No effect |
Ð |
Relaxation |
β2 |
Penis |
Erection |
M3 |
Ejaculation |
α |
Bladder detrusor |
Contraction |
|
Relaxation |
β2 |
Bladder sphincter |
Relaxation |
|
Contraction |
α1 |
TABLES IMPORTANT
149
PHARMACOLOGY IN 7 DAYS FOR MEDICAL STUDENTS
Table 7.3 Important ion channels and their stimulators and blockers
Ion channel |
Stimulator/s |
Blocker/s |
GABA-gated ClÐ channel |
Benzodiazepines |
Picrotoxin |
Renal tubular Na+ channel |
Aldosterone |
K+-sparing diuretics |
|
|
(amiloride, etc.) |
Voltage-gated Na+ channel |
Veratridine |
Local anaesthetics |
Voltage-gated Ca++ channel |
Dihydropyridines |
Ð |
|
β-agonists |
|
ATP-sensitive K+ channel |
Sulphonylureas |
ATP |
Table 7.4 Important enzyme-inhibiting drugs
Drug |
Enzyme inhibited |
Acetazolamide |
Carbonic anhydrase |
Aciclovir |
Thymidine kinase |
Allopurinol |
Xanthine oxidase |
Anti-HIV drugs (didanosine and zidovudine) |
Reverse transcriptase |
Aspirin |
Cyclooxygenase (COX) |
Captopril |
ACE |
Carbidopa |
Dopa decarboxylase |
Heparin |
Enzymes involved in blood clotting cascade |
Methotrexate |
Dihydrofolate reductase |
Neostigmine |
Acetylcholinesterase |
Organophosphorous compounds |
Acetylcholinesterase |
Selegiline |
MAO-B |
Simvastatin |
HMG-CoA reductase |
Trimethoprim |
Dihydrofolate reductase |
|
|
150
|
IMPORTANT TABLES |
|
|
Table 7.5 Important drugs that inhibit transport proteins |
|
|
|
Drug |
Transport protein inhibited |
|
|
Cocaine |
5HT and α2 presynaptic receptors (→ inhibition of reuptake of |
|
serotonin and noradrenaline respectively) |
Tricyclic |
5HT and α2 presynaptic receptors (→ inhibition of reuptake of |
antidepressants |
serotonin and noradrenaline respectively) |
Digoxin |
Na+/K+ ATPase pump (→ ↑ force of contraction, ↓ rate of AV nodal |
|
conduction) |
Loop diuretics |
Na+/K+/ClÐ co-transporter (along the thick ascending limb [TAL] of loop |
|
of Henle) → inhibition of NaCl reabsorption |
Omeprazole |
H+/K+-ATPase proton pump (along the luminal surface of gastric |
|
parietal cells) → total inhibition of HCl synthesis |
Probenecid |
Weak acid carrier (along the proximal convoluted tubule [PCT]) → |
|
inhibition of urate absorption from the PCT |
Table 7.6 Important drugs that undergo extensive Þrst-pass metabolism
CVS drugs:
¥Aspirin
¥Nitrates (GTN; isosorbide dinitrate)
¥Metoprolol
¥Propranolol
¥Verapamil
Respiratory drugs:
¥Salbutamol CNS drugs:
¥Levodopa
¥Morphine
Table 7.7 Important drugs that produce active metabolites
Drug |
Active/toxic metabolite |
Azathioprine |
Mercaptopurine |
Cortisone |
Hydrocortisone |
Diazepam |
Oxazepam |
Enalapril |
Enalaprilat |
Morphine |
Morphine 6-glucuronide |
Prednisone |
Prednisolone |
|
|
151
PHARMACOLOGY IN 7 DAYS FOR MEDICAL STUDENTS
Table 7.8 Important drugs that produce toxic metabolites
Drug |
Active/toxic metabolite |
Cyclophosphamide |
Acrolein |
Halothane |
Trißuoroacetic acid |
Paracetamol |
N-acetyl-p-benzoquinone imine |
|
|
Table 7.9 Drugs that are excreted primarily unchanged in urine
CVS:
¥Atenolol
¥Frusemide
¥Digoxin ANS:
¥Neostigmine Antibiotics:
¥Benzylpenicillin
¥Gentamicin
¥Oxytetracycline Immunomodulator:
¥Methotrexate
152
