NEET MDS Lessons
Pharmacology
Nimesulide
analgesic and antipyretic properties
Nimesulide is a relatively COX-2 selective, non-steroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties. Its approved indications are the treatment of acute pain, the symptomatic treatment of osteoarthritis and primary dysmenorrhoea in adolescents and adults above 12 years old.
Banned - not used
Methyl salicylate
also known as oil of wintergreen, betula oil, methyl ester) is a natural product of many species of plants Structurally, it is methylated salicylic acid It is used as an ingredient in deep heating rubs
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.
Osmotic diuretics
An osmotic diuretic is a type of diuretic that inhibits reabsorption of water and sodium. They are pharmacologically inert substances that are given intravenously. They increase the osmolarity of blood and renal filtrate.
Mechanism(s) of Action
1. Reduce tissue fluid (edema)
2. Reflex cardiovascular effect by osmotic retention of fluid within vascular space which increases blood volume (contraindicated with Congestive heart failure)
3. Diuretic effect
o Makes H2O reabsorption far more difficult for tubular segments insufficient Na & H2O capacity in distal segments
o Increased intramedullary blood flow (washout)
o Incomplete sodium recapture (asc. loop). this is indirect inhibition of Na reabsorption (Na stays in tubule because water stays)
o Net diuretic effect:
Tubular concentration of sodium decreases
Total amount of sodium lost amount increases
GFR unchanged or slightly increased
Toxicity
Circulatory overload, dilutional hyponatremia, Hyperkalemia, edema, skin necrosis
Agents
Mannitol
Aquaretics
An aquaretic is a class of drug that is used to promote aquaresis, the excretion of water without electrolyte loss.
Lithium, demeclocycline
Mechanism of Action
1. Block ADH action on distal tubule and collecting duct. Blocking ADH decreases H2O permeability. H2O is not recovered (distal tubule) using osmotic draw of counter-current multiplier so aquaretics reduce water reabsorption (tubule to blood stream).
2. Net effect is an increase in free water clearance
Gabapentin (Neurontin): newer; for generalized tonic-clonic seizures and partial seizures (partial and complex)
Mechanism: unknown but know doesn’t mimic GABA inhibition or block Ca currents
Side effects: dizziness, ataxia, fatigue; drug well-tolerated and no significant drug interactions
Heparin:
- Inhibits blood coagulation by forming complexes with an α2-globulin (Antithrombin III) and each of the activated proteases of the coagulation cascade (Kallikrein, XIIa, XIa, IXa, Xa, and Thrombin). After formation of the heparin-ATIII-coagulation factor, heparin is released and becomes available again to bind to free ATIII.
- Blocks conversion of Prothrombin to Thrombin and thus inhibits the synthesis of Fibrin from Fibrinogen.
- Inhibits platelet function and increases vascular permeability. May induce moderate to severe thrombocytopenia.
- Is prescribed on a “unit” basis.
- Heparin is not effective after oral administration and is generally administered by intravenous or subcutaneous injection. Intramuscular injections should be avoided.
- Heparin does not cross the placenta and does not pass into the maternal milk.
- is contraindicated in any situation where active bleeding must be avoided.
Ulcerative lesions, intracranial hemorrhage, etc.
Overdosage:
• Simple withdrawal.
• Protamine sulfate: Highly basic peptide that binds heparin and thus neutralizes its effects.