NEET MDS Lessons
Pharmacology
Barbiturates
1. Long-acting. Phenobarbital is used to treat certain types of seizures (see section on antiepileptic drugs).
2. Intermediate-acting. Amobarbital, pentobarbital (occasionally used for sleep), secobarbital.
3. Short-acting. Hexobarbital, methohexital, thiopental—rarely used as IV anesthetics.
Example calculations of maximum local anesthetic doses for a 15-kg child
Articaine
5 mg/kg maximum dose × 15 kg = 75 mg
4% articaine = 40 mg/mL
75 mg/(40 mg/mL) = 1.88 mL
1 cartridge = 1.8 mL
Therefore, 1 cartridge is the maximum
Lidocaine
7 mg/kg × 15 kg = 105 mg
2% lidocaine = 20 mg/mL
105 mg/(20 mg/mL) = 5.25 mL
1 cartridge = 1.8 mL
Therefore, 2.9 cartridges is the maximum
Mepivacaine
6.6 mg/kg × 15 kg = 99 mg
3% mepivacaine = 30 mg/mL
99 mg/(30 mg/mL) = 3.3 mL
1 cartridge = 1.8 mL
Therefore, 1.8 cartridges is the maximum.
Prilocaine
8 mg/kg × 15 kg = 120 mg
4% prilocaine = 40 mg/mL
120 mg/(40 mg/mL) = 3 mL
1 cartridge = 1.8 mL
Therefore, 1.67 cartridges is the maximum
Ampicillin offered a broader spectrum of activity than either of the original penicillins and allowed doctors to treat a broader range of both Gram-positive and Gram-negative infections. Ampicillin is often used in molecular biology as a test for the uptake of genes (e.g., by plasmids) by bacteria (e.g., E. coli)
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.)
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.
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.
Propofol -Intravenous Anesthetics
- A nonbarbiturate anesthetic
- It is very lipid-soluble, acts rapidly and has a short recovery time.
- It is associated with less nausea and vomiting than some of the other IV anesthetics.
- Propofol is very similar to thiopental in its effects on the cardiorespiratory system.
- It does not have any analgesic properties but lowers the dose of opioid needed when the two agents are used in combination.
- The most significant adverse cardiovascular effect associated with propofol administration is hypotension. It should be used with caution in patients with cardiac disease.