NEET MDS Lessons
Pharmacology
Methicillin
Methicillin is an antibiotic related to penicillin and other beta-lactam containing antibiotics. It is often used to treat infections caused by bacteria carrying an antibiotic resistance, e.g., staphylococci. As methicillin is deactivated by gastric acid, it has to be administered by injection.
Uses Methicillin serves a purpose in the laboratory to determine antibiotic sensitivity in microbiological culture.
Serotonin or 5-hydroxytryptamine (5-HT)
It is a neurotransmitter, widely distributed in the CNS, beginning in the midbrain and projecting into thalamus, hypothalamus, cerebral cortex, and spinal cord. CNS serotonin is usually an inhibitory neurotransmitter and is associated with mood, the sleep-wake cycle.
Serotonin is thought to produce sleep by inhibiting CNS activity.
In the blood, 5-HT is present in high concentration in platelets (regulator of platelets function) and also high concentration in intestine
Pharmacological effects:
Smooth muscles. 5-HT stimulates the G.I smooth muscle; it increases the peristaltic movement of intestine.
Serotonin contracts the smooth muscle of bronchi;
Blood vessels. If serotonin is injected i.v, the blood pressure usually first rises, because of the contraction of large vessels and then falls because of arteriolar dilatation. Serotonin causes aggregation of platelets.
Specific agonists
- Sumatriptan a selective 5-HT1D used in treatment of acute migraine.
- Buspirone a selective 5-HT1A used in anxiety.
- Ergotamine is a partial agonist used in migraine. It acts on 5-HT1A receptor.
Nonspecific 5-HT receptor agonist
o Dexfenfluramine used as appetite suppressant.
Specific antagonists
o Spiperone (acts on 1A receptor) and
o Methiothepin (acts on 1A, 1B, 1D receptors)
Heroin (diacetyl morphine)
Heroin is synthetically derived from the natural opioid alkaloid morphine
Largely owing to its very rapid onset of action and very short half-life, heroin is a popular drug of abuse
It is most effective when used intravenously
Heroin is rapidly deacetylated to 6-monoacetyl morphine and morphine, both of which are active at the mu opioid receptor
More lipid soluble than morphine and about 2½ times more potent. It enters the CNS more readily.
Factors affecting onset and duration of action of local anesthetics
pH of tissue
pKa of drug
Time of diffusion from needle tip to nerve
Time of diffusion away from nerve
Nerve morphology
Concentration of drug
Lipid solubility of drug
Kinins
Peptide that are mediated in the inflammation.
Action of kinin:
On CVS: vasodilatation in the kidneys, heart, intestine, skin, and liver. It is 10 times active than histamine as vasodilator.
On exocrine and endocrine glands: kinin modulate the tone of pancreas and salivery glands and help regulate GIT motility, also affect the transport of water and electrolytes, glucose and amino acids through epithelial cell transport.
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.
ANTIBIOTICS
Chemotherapy: Drugs which inhibit or kill the infecting organism and have no/minimum effect on the recipient.
Antibiotic these are substances produced by microorganisms which suppress the growth of or kill other micro-organisms at very low concentrations.
Anti-microbial Agents: synthetic as well as naturally obtained drugs that attenuate micro-organism.
SYNTHETIC ORGANIC ANTIMICROBIAL DRUGS
Sulfonamides
Trimethoprim-sulfamethoxazole
Quinolones – Ciprofloxacin
ANTIBIOTICS THAT ACT ON THE BACTERIAL CELL WALL
Penicillins
Cephalosporins
Vancomycin
INHIBITORS OF BACTERIAL PROTEIN SYNTHESIS
Aminoglycosides - Gentamicin
Antitubercular Drugs: Isoniazid & Rifampin
Tetracyclines
Chloramphenicol
Macrolides – Erythromycin, Azithromycin
Clindamycin
Mupirocin
Linezolid
ANTIFUNGAL DRUGS
Polyene Antibiotics (Amphotericin B, Nystatin and Candicidin)
Imidazole and Triazole Antifungal Drugs
Flucytosine
Griseofulvin
ANTIPROTOZOAL DRUGS
Antimalarial Drugs – Quinine, Chloroquine, Primaquine
Other Antiprotozoal Drugs – Metronidazole, Diloxanide, Iodoquinol
ANTIHELMINTHIC DRUGS
Praziquantel
Mebendazole
Ivermectin
ANTIVIRAL DRUGS
Acyclovir
Ribavirin
Dideoxynucleosides
Protease inhibitors