NEET MDS Lessons
Pharmacology
Thrombolytic Agents:
Tissue Plasminogen Activator (t-PA, Activase)
t-PA is a serine protease. It is a poor plasminogen activator in the absence of fibrin. t-PA binds to fibrin and activates bound plasminogen several hundred-fold more rapidly than it activates plasminogen in the circulation.
Streptokinase (Streptase)
Streptokinase is a protein produced by β-hemolytic streptococci. It has no intrinsic enzymatic activity, but forms a stable noncovalent 1:1 complex with plasminogen. This produces a conformational change that exposes the active site on plasminogen that cleaves a peptide bond on free plasminogen molecules to form free plasmin.
Urokinase (Abbokinase)
Urokinase is isolated from cultured human cells.Like streptokinase, it lacks fibrin specificity and therefore readily induces a systemic lytic state. Like t-PA, Urokinase is very expensive.
Contraindications to Thrombolytic Therapy:
• Surgery within 10 days, including organ biopsy, puncture of noncompressible vessels, serious trauma, cardiopulmonary resuscitation.
• Serious gastrointestinal bleeding within 3 months.
• History of hypertension (diastolic pressure >110 mm Hg).
• Active bleeding or hemorrhagic disorder.
• Previous cerebrovascular accident or active intracranial bleeding.
Aminocaproic acid:
Aminocaproic acid prevents the binding or plasminogen and plasmin to fibrin. It is a potent inhibitor for fibrinolysis and can reverse states that are associated with excessive fibrinolysis.
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
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.
A. Sympathetic Nervous System Depressants
1. Antagonists
Both α-adrenoceptor antagonists and β-adrenoceptor antagonists are useful antihypertensives.
- α-blocker Prazosin, phentolamine, phenoxybenzamine
- β-blocker Propranolol ,Metoprolol, atenolol
- α/β-blocker labetalol
2. Sympathetic depressants
a. Examples of peripherally acting agents include
- reserpine This agent interferes with the storage of norepinephrine
- quanethidine This agent interferes with the release of norepinephrine
- trimethaphan This agent blocks transmission through autonomic ganglia.
b. Examples of Centrally acting agents include
- alphamethyldopa
- clonidine. These agents act by decreasing the number of impresses along sympathetic nerves.
Adverse Effect
include nasal congestion, postural hypotension, diarrhea, sexual dysfunction, dry mouth. sedation and drowsiness.
B. Directly Acting Vasodilators
Act on vascular smooth muscle cells independently of adrenergic nerves and adrenergic receptors.
Relaxation of vascular smooth muscle which leads to a decrease in peripheral vascular resistance.
Sites of action of vasodilators are many. For example
Calcium Channel Blocker’s MOA
. Decrease automaticity & conduction thru SA & AV nodes
. Decreased myocardial contractility
. Decreased peripheral & coronary
smooth muscle tone = decrease SVR
Potassium channels activators
minoxidil, cause vasodilation by activating potassium channels in vascular smooth muscle.
An increase in potassium conductance results in hyperpolarization of the cell membrane which is associated with relaxation of smooth muscle.
Nitrovasodilators, such as sodium nitroprusside,
Increase in intracellular cGMP. cGMP in turn activates a protein kinase. Directly-Acting Vasodilators are on occasion used alone but more frequently are used in combination with antihypertensive agents from other classes (esp. a β-blocker and a diuretic.)
Needle selection
Nerve blocks:
Inferior alveolar- 25 G short (LLU technique)
PSA- 25 G short
Mental/Incisive- 25 G short
Palatal- 27/30 G short/ultrashort
Gow-Gates/Akinosi- 25 G long
Infraorbital- 25 G long
Field Block:
ASA 25/27 short
Infiltration:
Infiltration/SP 25/27 short
PDL/Intraosseous
PDL 27/30 short
Intraosseous 30 short/ultrashort
Oxytetracycline
Treats Oxytetracycline is a medicine used for treating a wide range of infections including infections of the lungs, urinary system, skin and eyes. It may also be used to treat sexually transmitted infections, infections caused by lice, rickettsial infections, cholera and plague. It is very occasionally used to treat leptospirosis, gas gangrene, and tetanus.
Nitrous Oxide (N2O)
MAC 100%, blood/gas solubility ratio 0.47
- An inorganic gas., low solubility in blood, but greater solubility than N2
- Inflammable, but does support combustion.
- Excreted primarily unchanged through the lungs.
- It provides amnesia and analgesia when administered alone.
- Does not produce muscular relaxation.
- Less depressant to both the cardiovascular system and respiratory system than most of the other inhalational anesthetics.
- Lack of potency and tendency to produce anoxia are its primary limitations.
- The major benefit of nitrous oxide is its ability to reduce the amount of the secondary anesthetic agent that is necessary to reach a specified level of anesthesia.