NEET MDS Lessons
Pharmacology
Fourth Generation:
These are extended spectrum antibiotics. They are resistant to beta lactamases.
Cefipime
Monoamine oxidase inhibitors (MAOIs)
e.g. phenelzine, tranylcypromine, moclobemide
- Belong to first generation antidepressants with TCAs
- Most MAOIs irreversibly inhibit the intraneuronal catabolism of norepinephrine and serotonin by MAO-A and MAO-B
- increase brain levels of noradrenaline and 5-HT
- Moclobemide causes selective, reversible inhibition of MAO-A
DRUG INTERACTIONS
Hypertensive crises similar to cheese reaction with OTC cough/cold preparations containing indirect-sympathomimetics
e.g. ephedrine
- Other antidepressants should not be started at least 2 weeks after stopping MAOIs and vice versa due to risk of serotonin syndrome
- Similar interaction with pethidine
ADVERSE DRUG REACTIONS
- Antimuscarinic side effects (e.g. dry mouth, blurred vision, urinary retention)vision, urinary retention)
- Excessive central stimulation causes tremors, excitement and insomnia
- Postural hypotension
- Increased appetite with weight gain
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
Etomidate -Intravenous Anesthetics
- A nonbarbiturate anesthetic used primarily to induce surgical anesthesia.
- It does not produce analgesia.
- Etomidate has minimal effect on the cardiovascular system and respiration during induction of anesthesia.
- Like the barbiturates, etomidate decreases cerebral blood flow, cerebral metabolic rate and intracranial pressure.
- No changes in hepatic, renal or hematologic function have been reported.
- Myoclonic muscle movements are relatively common.
- Postoperative nausea and vomiting are more common with etomidate than with barbiturates.
Nystatin
Candida spp. are sensitive to nystatin.
Uses: Cutaneous, vaginal, mucosal and esophageal infections.
Candida infections can be treated with nystatin.
Cryptococcus is also sensitive to nystatin.
Nystatin is often used as prophylaxis in patients who are at risk for fungal infections, such as AIDS patients with a low CD4+ count and patients receiving chemotherapy.
MOA
nystatin binds to ergosterol, the main component of the fungal cell membrane. When present in sufficient concentrations, it forms a pore in the membrane that leads to K+ leakage and death of the fungus.
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
Sulfonylureas
1st generation
tolbutamide
chlorpropamide
2nd generation
glyburide
glimepiride
glipizide
Mechanism
glucose normally triggers insulin release from pancreatic β cells by increasing intracellular ATP
→ closes K+ channels → depolarization → ↑ Ca2+ influx → insulin release
sulfonylureas mimic action of glucose by closing K+ channels in pancreatic β cells
→ depolarization → ↑ Ca2+ influx → insulin release
its use results in
↓ glucagon release
↑ insulin sensitivity in muscle and liver
Clinical use
type II DM
stimulates release of endogenous insulin
cannot be used in type I DM due to complete lack of islet function
Toxicity
first generation
disulfiram-like effects
especially chlorpropamide
second generation
hypoglycemia
weight gain