NEET MDS Lessons
Pharmacology
Procaine penicillin Procaine penicillin is a combination of benzylpenicillin with the local anaesthetic agent procaine. This combination is aimed at reducing the pain and discomfort associated with a large intramuscular injection of penicillin.
Indications
respiratory tract infections where compliance with oral treatment is unlikely ,syphilis, cellulitis
Anticonvulsants: include carbamazepine (use when lithium not tolerated; may not be as effective) .
valproic acid (use when lithium not tolerated; rapid onset)
Agonist, Antagonist, and Partial Agonists
Agonists: molecules that activate receptors. A drug that mimics the body's own regulatory processes.
Antagonists: produce their effects by preventing receptors activation by endogenous regulatory molecules and drugs. Block activation of receptors by agonists.
Noncompetive Antagonist: Bind irreversibly to receptors, and reduce the maximal response that an agonist can elicit.
Competitive Antagonist: Bind reversibly to receptors, competing with agonists for binding sites.
Partial Agonists: Have moderate intrinsic activity, the maximal effect that a partial agonist can produce is lower than that of a full agonist. Act as antagonists as well as agonists.
Fentanyl (Sublimaze)
- Related chemically to meperidine.
- Approximately 80 times more potent than morphine.
- Duration of action very short (t1/2 20 min).
- Used mainly following general anesthesia.
- Neurolept analgesia: Fentanyl & Droperidol (Innovar)
- fentanyl in analgesic (2-10 µg/kg), or anaesthetic (30-100 µg/kg) doses seldom causes significant decreases in blood pressure when given alone, even in patients with poor LV function
- hypotension following fentanyl is mostly due to bradycardia and can be prevented by the use of anticholinergics, sympathomimetics or agents such as pancuronium this is more likely to occur in patients with high pre-existing sympathetic tone
- hypertension is the commonest disturbance with high dose fentanyl anaesthesia, usually accompanying intubation, sternotomy, or aortic root dissection
Serotonin-norepinephrine reuptake inhibitors(SNRIs)
e.g. venlafaxine and duloxetine
- Inhibit the reuptake of both 5-HT and norepinephrine
- Has a more favourable adverse effect profile than TCAs
Norepinephrine reuptake inhibitor
e.g. bupropion, reboxetine
Monoamine receptor antagonists
e.g. mirtazapine, trazodone, mianserin
Class III Potassium Channel Blockers
Prolong effective refractory period by prolonging Action Potential
Treatment: ventricular tachycardia and fibrillation, conversion of atrial fibrillation or flutter to sinus rhythm, maintenance of sinus rhythm
– Amiodarone (Cordarone) – maintenance of sinus rhythm
– Bretylium (Bretylol)
– Ibutilide (Corvert)
– Dofetilide (Tykosyn)
– Sotalol (Betapace)
Amiodarone
- Has characteristics of sodium channel blockers, beta blockers, and calcium channel blockers
- Has vasodilating effects and decreases systemic vascular resistance
- Prolongs conduction in all cardiac tissue
- Decreases heart rate
- Decreases contractility of the left ventricles
Class III - Adverse Effects
- GI- Nausea vomiting and GI distress
- CNS- Weakness and dizziness
- CV-Hypotension, CHF, and arrhythmias are common.
- Amiodarone associated with potentially fatal Hepatic toxicity, ocular abnormalities and serious cardiac arrhythmias.
Drug – Drug Interactions
These drugs can cause serious toxic effects if combined with digoxin or quinidine.
Mefenamic acid
Analgesic, anti‐inflammatory properties less effective than aspirin
Short half‐lives, should not be used for longer than one week and never in pregnancy and in children.
Enhances oral anticoagulants
Used to treat pain, including menstrual pain. It decreases inflammation (swelling) and uterine contractions.