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Pharmacology - NEETMDS- courses
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Pharmacology

Antihypertensives Drugs

CATEGORIES
I.    Diuretics to reduce blood volume 
Chlorothiazide (Diuril)

II. Drugs that interfere with the Renin-Angiotensin System

A. Converting enzyme inhibitors             Captopril , enalapril, Lisinopril

B. Angiotensin receptor antagonists         Saralasin Losartan 

III. Decrease peripheral vascular resistance and/or cardiac output

A. Directly acting vasodilators
1. calcium channel blockers           Nifedipine , Diltiazem,  amlodipine

2. potassium channel activators     Minoxidil 

3. elevation of cGMP                      Nitroprusside 

4. others                                         Hydralazin e

B. Sympathetic nervous system depressants

1. α-blockers                             Prazosin, phentolamine, phenoxybenzamine

2. β-blockers                             Propranolol ,Metoprolol, atenolol

3. norepinephrine synthesis inhibitors     Metyrosine 

4. norepinephrine storage inhibitors     Reserpine
 
5. transmitter release inhibitors         Guanethidine 

6. centrally acting: decrease 
sympathetic outflow
                    Clonidine , methyldopa

Uses of NSAIDs

NSAIDs are usually indicated for the treatment of acute or chronic conditions where pain and inflammation are present. Research continues into their potential for prevention of colorectal cancer, and treatment of other conditions, such as cancer and cardiovascular disease.

NSAIDs are generally indicated for the symptomatic relief of the following conditions.

rheumatoid arthritis, osteoarthritis, inflammatory arthropathies (e.g. ankylosing spondylitis, psoriatic arthritis, Reiter's syndrome), acute gout, dysmenorrhoea, metastatic bone pain ,headache and migraine, postoperative pain, mild-to-moderate pain due to inflammation and tissue injury, pyrexia, renal colic

Aspirin, the only NSAID able to irreversibly inhibit COX-1, is also indicated for inhibition of platelet aggregation; an indication useful in the management of arterial thrombosis and prevention of adverse cardiovascular events.

Levofloxacin

Levofloxacin is effective against a number of gram-positive and gram-negative bacteria. Because of its broad spectrum of action, levofloxacin is frequently prescribed in hospitals for pulmonary infections

Ketoconazole

synthetic antifungal drug

used for infections such as  athlete's foot, ringworm, candidiasis (yeast infection or thrush), jock itch.

Ketoconazole is used to treat eumycetoma, the fungal form of mycetoma.

MOA: Ketoconazole is imidazole structured, and interferes with the fungal synthesis of  ergosterol, the main constituent of cell membranes, as well as certain enzymes. It is specific for fungi, as mammalian cell membranes contain no ergosterol.

Sensitive fungi Ketoconazole inhibits growth of  dermatophytes and  yeast species (such as Candida albicans).

Clavulanic acid is often combined with amoxicillin to treat certain infections caused by bacteria, including infections of the ears, lungs, sinus, skin, and urinary tract. It works by preventing bacterium that release beta-lactamases from destroying amoxicillin.

SULPHONAMIDES

Derivative of  sulphonilamide (Para-amino Benzene (PABA ) sulphonamide).

Anti-bacterial spectrum

Bacteriostatic to gram + and gram - bacteria. but bactericidal concentrations arce attained in urine. S pyogencs. H influenzae.E coli, few- Staph aureus. gonococci. pneumococci, proteus, shigella and Lymphogranuloma venereum.

Mechanism of action

Inhibits bacterial folate synthetase as they compete with PABA

Less soluble in acid urine and may precipitate to cause crystalluria.

Accumulate in patients with renal failure and can cause toxicity

Classification

Shart Acting (4-8 Hrs) sulphadiazine, sulphamethizole.

Intermediate acting(8-16 Hrs): sulphamethoxazole , sulphaphenazole

Long Acting(l-7days): sulphamethoxypyridazine.

Ultralong Acting(3-8days): sulfaline

Adverse effects

I. nausea, vomiting and epigastric pain

2. crystalluria

3. hypersensitivity-like polyarthritis nodosa. Steven-Johnson Syndrome. photosenstivity

4.hemolysis in G-6PD deficiency

5. kernicterus

They inhibit metabolism of phenytoin. tolbutamide. methotrexate

Therapeutic Use

UTI Meningitis, Streptococcal pharyngitis, Bacillary Dysentery

Antiplatelet Drugs:

Whereas the anticoagulant drugs such as Warfarin and Heparin suppress the synthesis or activity of the clotting factors and are used to control venous thromboembolic disorders, the antithrombotic drugs suppress platelet function and are used primarily for arterial thrombotic disease. Platelet plugs form the bulk of arterial thrombi.

Acetylsalicylic acid (Aspirin)

• Inhibits release of ADP by platelets and their aggregation by acetylating the enzymes (cyclooxygenases or COX) of the platelet that synthesize the precursors of Thromboxane A2 that is a labile inducer of platelet aggregation and a potent vasoconstrictor.

• Low dose (160-320 mg) may be more effective in inhibiting Thromboxane A2 than PGI2 which has the opposite effect and is synthesized by the endothelium.

• The effect of aspirin is irreversible.

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