NEET MDS Lessons
Pharmacology
COAGULANTS
An agent that produces coagulation (Coagulation is a complex process by which blood forms clots).
ANTICOAGULANTS
An anticoagulant is a substance that prevents coagulation; that is, it stops blood from clotting.
Anticoagulants:
Calcium Chelators (sodium citrate, EDTA)
Heparin
Dalteparin Sodium (Fragmin) -Low molecular-weight heparin
Enoxaparin - Low molecular-weight heparin
Tinzaparin Sodium - Low molecular-weight heparin
Warfarin
Lepirudin - recombinant form of the natural anticoagulant hirudin: potent and specific Thrombin inhibitor
Bivalirudin - analog of hirudin: potent and specific Thrombin inhibitor
Procoagulants:
Desmopressin acetate
Antiplatelet Drugs:
Acetylsalicylic Acid, Ticlopidine, Sulfinpyrazone, Abciximab , Clopidogrel bisulfate
Fibrinolytic Drugs:
Tissue Plasminogen Activator (t-PA, Activase), Streptokinase (Streptase),
Anistreplase, Urokinase
Antagonists:
Protamine sulfate, Aminocaproic acid
Pharmacological agents used to treat blood coagulation disorders fall in to three major categories:
1. Anticoagulants: Substances that prevent the synthesis of a fibrin network which inhibits coagulation and the formation of arterial thrombi and thromboembolic clots.
2. Antiplatelet agents: Substances that reduce the adhesion and aggregation of platelets.
3. Fibrinolytic agents: Substances that promote the destruction of already formed blood clots or thrombi by disrupting the fibrin mesh.
Estimation of the risk of anesthesia (American Society of Anesthesiologists scale)
• ASA 1: healthy patient.
• ASA 2: patient with stable, treated illness like arterial hypertension, diabetes melitus, asthma bronchiale, obesity
• ASA 3: patient with systemic illness decreasing sufficiency like heart illness, late infarct
• ASA 4: patient with serious illness influencing his state like renal insuficiency, unstable hypertension, circulatory insuficiency
• ASA 5: patient in life treatening illness
• ASA 6: brain death- potential organ donor
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
Ibuprofen
used to relieve the symptoms of arthritis, primary dysmenorrhoea, fever; and as an analgesic, especially where there is an inflammatory component.
Indications
rheumatoid arthritis, osteoarthritis, juvenile rheumatoid arthritis, primary dysmenorrhoea
fever, relief of acute and/or chronic pain states in which there is an inflammatory component
MOA
inhibition of cyclooxygenase (COX); thus inhibiting prostaglandin synthesis.
Ether (diethylether)
Ether (diethylether) MAC 2.0%, Blood/gas solubility ratio 15
- Ether is generally mixed with 3% ethanol to retard oxidation. Peroxides form on exposure to air and can enhance the danger of an explosion.
- Slow rate of induction and recovery due to its high blood/gas solubility ratio.
- Produces profound muscular relaxation.
- Both the rate and the minute volume of ventilation tend to be elevated during the inhalation of ether.
- Ether maintains good circulatory stability and does not sensitize the heart to the arrhythmogenic action of catecholamines.
- More than 90% of the absorbed ether can be recovered unchanged in the expired air. Metabolism is not extensive and the metabolites are not hepatotoxic.
- Ether is a versatile anesthetic of unexcelled safety, but it is flammable and irritating to breathe. Secretions can be blocked with anticholinergics.
Cells of the Nervous System
1-Neurons (Nerve Cells):function units of the nervous system by conducting nerve impulses, highly specialized and amitotic. Each has a cell body (soma), one or more dendrites, and a single axon.
• Cell Body: it has a nucleus with at least one nucleolus and many of the typical cytoplasmic organelles, but lacks centriolesfor cell division.
• Dendrites:Dendrites and axons are cytoplasmic extensions (or processes), that project from the cell body. They are sometimes referred to as fibers. Dendrites (afferent processes) increase their surface area to receive signals from other neurons, and transmit impulses to the neuron cell body.
• Axon: There is only one axon (efferent process) that projects from each cell body.
It carries impulses away from the cell body.
2-Glial cells: do not conduct nerve impulses, but support, nourish, and protect the neurons. They are mitotic, and far more numerous than neurons.
Astrocyte: A glialcell that provides support for neurons of the CNS, provides nutrients regulates the chemical composition of the extracellularfluid.
• Oligodendrocyte: A type of glialcell in the CNS that forms myelin sheaths.
• Microglia:The smallest glialcells; act as phagocytes (cleaning up debris) and protect the brain from invading microorganisms.
• Schwann cell:A cell in the PNS that is wrapped around a myelinatedaxon, providing one segment of its myelin sheath.
Diclofenac
Short half life (1‐2 hrs), high 1stpass metab., accumulates in synovial fluid after oral admn., reduce inflammation, such as in arthritis or acute injury
Mechanism of action
inhibition of prostaglandin synthesis by inhibition of cyclooxygenase (COX). There is some evidence that diclofenac inhibits the lipooxygenase pathways, thus reducing formation of the
leukotrienes (also pro-inflammatory autacoids). There is also speculation that diclofenac may inhibit phospholipase A2 as part of its mechanism of action. These additional actions may explain the high potency of diclofenac - it is the most potent NSAID on a molar basis.
Inhibition of COX also decreases prostaglandins in the epithelium of the stomach, making it more sensitive to corrosion by gastric acid. This is also the main side effect of diclofenac and other drugs that are not selective for the COX2-isoenzyme.