NEET MDS Lessons
Pharmacology
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.
Carbapenems: Broadest spectrum of beta-lactam antibiotics.
imipenem with cilastatin
meropenem
ertapenem
Monobactams: Unlike other beta-lactams, there is no fused ring attached to beta-lactam nucleus. Thus, there is less probability of cross-sensitivity reactions.
aztreonam
Beta-lactamase Inhibitors No antimicrobial activity. Their sole purpose is to prevent the inactivation of beta-lactam antibiotics by beta-lactamases, and as such, they are co-administered with beta-lactam antibiotics.
clavulanic acid
tazobactam
sulbactam
Benzodiazepines
All metabolites are active sedatives except the final glucuronide product.
Elimination half-life varies a great deal from drug to drug.
?-Hydroxylation is a rapid route of metabolism that is unique to triazolam,
midazolam, and alprazolam.
This accounts for the very rapid metabolism and short sedative actions of these
drugs.
Pharmacological effects of benzodiazepines
- Antianxiety.
- Sedation.
- Anticonvulsant (including drug-induced convulsions).
- Amnesia, especially drugs like triazolam.
- Relax skeletal muscle (act on CNS polysynaptic pathways).
Indications
- IV sedation, (e.g., midazolam, diazepam, lorazepam).
- Antianxiety.
- Sleep induction.
- Anticonvulsant (e.g., diazepam, clonazepam).
- Panic disorders.
- Muscle relaxation.
Adverse effects
- Ataxia, confusion.
- Excessive sedation.
- Amnesia (not a desired effect with daytime sedation).
- Altered sleep patterns (increase stage 2 and decrease stage 4 sleep).
Valdecoxib
used in the treatment of osteoarthritis, acute pain conditions, and dysmenorrhoea
Etoricoxib new COX-2 selective inhibitor
PHARYNGEAL DEMULCENTS
Administered in the form of lozenges, cough drops and cough linctus.
Produce soothing action on throat directly and by increasing the flow of saliva and provide symptomatic relief from dry cough.
EXPECTORANT
Expectorants are the drugs which increase the production of bronchial secretion and reduce its viscosity to facilitate its removal by coughing.
ANTITUSSIVES
They are central cough suppressants and act centrally to raise the threshold of cough centre and inhibit the cough reflex by suppressing the coordinating cough centre in the medulla oblongata.
Codeine - it depresses cough centre but is less constipating and abuse liability is low.
Pholcodeine is similar to codeine in efficacy and is longer acting. It has no analgesic or addicting property.
Noscapine is another opium alkaloid of benzylisoquinoline group. It is used as antitussive with no analgesic and drug abuse or drug dependence property.
Dextromethorphan is a synthetic compound and its dextroisomer is used as antitussive and is as effective as codeine
Pipazethate is another synthetic compound of phenothiazine category used as antitussive with little analgesic and sedative properties.
ANTIHISTAMINICS
They do not act on cough centre but provide relief due to their sedative and anticholinergic action.
BRONCHODILATORS
Bronchodilators are helpful in individuals with cough and bronchoconstriction due to bronchial hyperreactivity. They help by improving the effectiveness of cough in clearing secretions.
NSAIDs: Classification by Plasma Elimination Half Lives
Short Half Life (< 6 hours):
more rapid effect and clearance
• Aspirin (0.25-0.33 hrs),
• Diclofenac (1.1 ± 0.2 hrs)
• Ketoprofen (1.8± 0.4 hrs),
• Ibuprofen (2.1 ± 0.3 hrs)
• Indomethacin (4.6 ± 0.7 hrs)
Long Half Life (> 10 hours):
slower onset of effect and slower clearance
• Naproxen (14 ± 2 hrs)
• Sulindac (14 ± 8 hrs),
• Piroxicam (57 ± 22 hrs)
Ketoprofen
It acts by inhibiting the body's production of prostaglandin.