NEET MDS Lessons
Pharmacology
Rofecoxib
Inhibit prostacyclin(PGI2) in vascular endothelium , letting TXA2 act freely and promote platelet aggregation.
used in the treatment of osteoarthritis, acute pain conditions, and dysmenorrhea
Higher incidence of cardiovascular thrombotic events.
Not used due to increase risk of heart attack, stroke
OXYMETAZOLINE
It is a directly acting sympathomimetic amine used in symptomatic relief in nasal congestion which increases mucosal secretion.
It is used:
- As a nasal decongestant in allergic rhinitis, with or without the addition of antazoline or sodium chromoglycate.
- As an ocular decongestant in allergic conjunctivitis.
Compounds like naphazoline and xylometazoline are relatively selective α2 agonists, which on topical application produce local vasoconstriction.
Antidiarrheal
Antidiarrheal drugs may be given to relieve the symptom (non-specific therapy) or may be given to treat the underlying cause of the symptom (specific therapy).
Ι. Drugs used for the symptomatic (non-specific) treatment of diarrhoea include:
• Opiates and opiate derivatives are the most effective (such as morphine), but it is not used because of potentially serious adverse effects. Other agents, such as diphenoxylate and loperamide, are commonly used.
• Adsorbent – demulcent products such as kaolin – pectin preparation may be included in antidiarrheal preparations. Unfortunately, they may adsorb nutrients and other drugs, including the antidiarrheal agents if given concurrently.
• Anticholinergic agents e.g. atropine is occasionally used to decrease abdominal cramping and pain associated with diarrhoea.
ΙΙ. Specific therapy may include the use of antibacterial agents that are recommended for use in carefully selected cases of bacterial enteritis. For example, severe diarrhoea by salmonella, shigella, campylobacter and clostridia species can be treated by antibiotics (ampicillin, chloramphenicol, co-trimoxazole).
Valproic acid: broad spectrum (for most seizure types)
Mechanism: blocks Ca T currents in thalamic neurons (prevents reverberating activity in absence seizures), ↓ reactivation of Na channels (in tonic/clonic seizures; prolongs refractory periods of neurons, prevents high frequency cell firing)
Side effects: very low toxicity; common = anorexia, N/V; at high doses inhibits platelet function (bruising and gingival bleeding); rarely see idiosyncratic hepatotoxicity
Drug interactions: induces hepatic microsomal enzymes (↓ effectiveness of other drugs), binds tightly to plasma proteins so displaces other drugs
Doxycycline
Commonly prescribed for infections and to treat acne. treat urinary tract infections, gum disease, and other bacterial infections such as gonorrhea and chlamydia., as a prophylactic treatment for infection by Bacillus anthracis (anthrax). It is also effective against Yersinia pestis and malaria.
Classification
1. Natural Alkaloids of Opium
Phenanthrenes -> morphine, codeine, thebaine
Benzylisoquinolines -> papaverine, noscapine
2. Semi-synthetic Derivatives
diacetylmorphine (heroin) hydromorphone, oxymorphone hydrocodone, oxycodone
3. Synthetic Derivatives
phenylpiperidines pethidine, fentanyl, alfentanyl, sufentnyl
benzmorphans pentazocine, phenazocine, cyclazocine
propionanilides methadone
morphinans levorphanol
Dental implications of these drugs:
1. Adverse effects: gingival hyperplasia (phenytoin), osteomalacia (phenytoin, Phenobarbital), blood dyscrasias (all but rare)
2. Drug interactions: additive CNS depression (anesthetics, anxiolytics, opioid analgesics), induction of hepatic microsomal enzymes (phenytoin, Phenobarbital, carbamazepine), plasma protein binding (phenytoin and valproic acid)
3. Seizure susceptibility: stress can → seizures