NEET MDS Lessons
Pharmacology
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
ISOPRENALINE
It is beta-receptor stimulant, which stimulates the heart and causes tachycardia.
It relaxes the smooth muscles particularly the bronchial and GIT. It is mainly used in bronchial asthma, in the treatment of shock and as a cardiac stimulant in heart block.
ORCIPRENALINE
Is a potent β-adrenergic agonist.
Receptor sites in the bronchi and bronchioles are more sensitive to the drug than those in the heart and blood vessels.
AMPHETAMINE
increases the systolic and diastolic blood pressure. Amphetamine is a potent CNS stimulant and causes alertness, insomnia, increased concentration, euphoria or dysphoria and increased work capacity.
Amphetamines are drugs of abuse and can produce behavioural abnormalities and can precipitate psychosis.
PHENYLEPHRINE
It is used as a nasal decongestant and mydriatic agent and also in the treatment of paroxysmal supraventricular tachycardia.
UTERINE RELAXANTS (TOCOLYTICS)
ISOXSUPRINE
Isoxsuprine has a potent inhibitory effect on vascular and uterine smooth muscle and has been used in the treatment of dysmenorrhoea, threatened abortion, premature labour and peripheral vascular diseases.
Isoflurane (Forane) MAC 1.3%, Blood/gas solubility ratio 1.4
- Better muscle relaxation than with the other halogenated anesthetic agents.
- Isoflurane markedly potentiates the action of the neuromuscular blocking agents.
- Produces rapid onset and recovery of anesthesia.
- Does not sensitize the heart to catecholamines.
- Produces respiratory depression, but produces less cardiovascular depression
- than does halothane.
- It has an extremely low degree of metabolism and is apparently relatively
- nontoxic.
Treatment modifications to consider if there are concerns regarding vasoconstrictors
- Monitor blood pressure and heart rate preoperatively
- Minimize administration of epinephrine or levonordefrin
- Monitor blood pressure and heart rate 5 min after injection
- May re-administer epinephrine or levonordefrin if blood pressure and heart rate are stable
- Continue to monitor as required
- Consider limiting epinephrine to 0.04 mg, levonordefrin to 0.2 mg
- Avoid epinephrine 1:50,000
- Never use epinephrine-impregnated retraction cord
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.
Amphotericin B
Main use is in systemic fungal infections (e.g. in immunocompromised patients), and in visceral leishmaniasis. Aspergillosis, cryptococcus infections (e.g. meningitis) and candidiasis are treated with amphotericin B. It is also used empirically in febrile immunocompromised patients who do not respond to broad-spectrum antibiotics.
MOA:
As with other polyene antifungals, amphotericin B associates with ergosterol, a membrane chemical of fungi, forming a pore that leads to K+ leakage and fungal cell death
Side effects: nephrotoxicity (kidney damage) , headache, vomiting, convulsions and fever
The side-effects are much milder when amphotericin B is delivered in liposomes
Calcium Channel Blocking Agents
• Act on contractile and conductive tissues of the heart and on vascular smooth muscles
• Prevent movement of extracellular calcium into the cell
– Coronary and peripheral arteries dilate
– Myocardial contractility decreases
– Depress conduction system
Therapeutic Actions
• Inhibit movement of calcium ions across the membranes of myocardial and arterial muscle cells. Altering the action potential and blocking muscle cell contraction
• Depress myocardial contractility
• Slow cardiac impulse formation in the conductive tissues
• Cause a fall in BP