NEET MDS Lessons
Pharmacology
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
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.
Roxithromycin
It is used to treat respiratory tract, urinary and soft tissue infections. Roxithromycin is derived from erythromycin, containing the same 14-membered lactone ring. However, an N-oxime side chain is attached to the lactone ring.
Roxithromycin has similar antimicrobial spectrum as erythromycin, but is more effective against certain gram-negative bacteria, particularly Legionella pneumophilae.
When taken before a meal, roxithromycin is very rapidly absorbed, and diffused into most tissues and Phagocytes Only a small portion of roxithromycin is metabolised. Most of roxithromycin is secreted unchanged into the bile and some in expired air
Cells of the Nervous System
1-Neurons (Nerve Cells):function units of the nervous system by conducting nerve impulses, highly specialized and amitotic. Each has a cell body (soma), one or more dendrites, and a single axon.
• Cell Body: it has a nucleus with at least one nucleolus and many of the typical cytoplasmic organelles, but lacks centriolesfor cell division.
• Dendrites:Dendrites and axons are cytoplasmic extensions (or processes), that project from the cell body. They are sometimes referred to as fibers. Dendrites (afferent processes) increase their surface area to receive signals from other neurons, and transmit impulses to the neuron cell body.
• Axon: There is only one axon (efferent process) that projects from each cell body.
It carries impulses away from the cell body.
2-Glial cells: do not conduct nerve impulses, but support, nourish, and protect the neurons. They are mitotic, and far more numerous than neurons.
Astrocyte: A glialcell that provides support for neurons of the CNS, provides nutrients regulates the chemical composition of the extracellularfluid.
• Oligodendrocyte: A type of glialcell in the CNS that forms myelin sheaths.
• Microglia:The smallest glialcells; act as phagocytes (cleaning up debris) and protect the brain from invading microorganisms.
• Schwann cell:A cell in the PNS that is wrapped around a myelinatedaxon, providing one segment of its myelin sheath.
DOBUTAMINE
It is a derivative of dopamine and has relatively β1 -selective action and it also activates α1 receptors and do not have D1 receptor agonistic property. It increases the force of myocardial contraction and cardiac output without significant change in heart rate, blood pressure and peripheral resistance. It is used as inotropic agent and for short term management of CHF and also in patients who are unresponsive to digitalis.
Meperidine (Demerol)
Meperidine is a phenylpiperidine and has a number of congeners. It is mostly effective in the CNS and bowel
- Produces analgesia, sedation, euphoria and respiratory depression.
- Less potent than morphine, 80-100 mg meperidine equals 10 mg morphine.
- Shorter duration of action than morphine (2-4 hrs).
- Meperidine has greater excitatory activity than does morphine and toxicity may lead to convulsions.
- Meperidine appears to have some atropine-like activity.
- Does not constrict the pupils to the same extent as morphine.
- Does not cause as much constipation as morphine.
- Spasmogenic effect on GI and biliary tract smooth muscle is less pronounced than that produced by morphine.
- Not an effective antitussive agent.
- In contrast to morphine, meperidine increases the force of oxytocin-induced contractions of the uterus.
- Often the drug of choice during delivery due to its lack of inhibitory effect on uterine contractions and its relatively short duration of action.
- It has serotonergic activity when combined with monoamine oxidase inhibitors, which can produce serotonin toxicity (clonus, hyperreflexia, hyperthermia, and agitation)
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