NEET MDS Lessons
Pharmacology
Stimulants:
Amphetamines: amphetamine is a substrate of serotonin and NE uptake transporters so in cytoplasm, it competes for transport into storage vesicles → ↑ [ ] in cytoplasm then excess amines bind to membrane transporter and are transported out of cell
Drugs:
a. Dextroamphetamine: psychomotor stimulant (↓ fatigue), short-term weight loss, prevents narcolepsy
b. Methylphenidate (Ritalin): prevents narcolepsy, treatment for ADD and ADHD
c. Methamphetamine: psychomotor stimulant, abused widely (cheap, easy to make)
Side effects:
a. CNS: euphoria, anxiety, agitation, delirium, paranoia, panic, suicidal/homicidal impulses, psychoses, tolerance (develops rapidly to most CNS effects), physical dependence (not clinically relevant)
b. CV: headache, chills, arrhythmias and HTN (may be fatal)
Insulin
Insulin is only given parenterally (subcutaneous or IV) Various preparations have different durations of action
|
Preparation |
Onset (hrs) |
Peak (hrs) |
Duration (hrs) |
| Lispro (rapid-acting) | 15 min | 0.5-1.5 | 3-4 |
| Regular (short-acting) | 0.5-1 | 2-4 | 5-7 |
| NPH (intermediate) | 1-2 | 6-12 | 18-24 |
| Glargine (long-acting) | 1 | None | >24 |
Mechanism
bind transmembrane insulin receptor
activate tyrosine kinase
phosphorylate specific substrates in each tissue type
liver
↑ glycogenesis
store glucose as glycogen
muscle
↑ glycogen and protein synthesis
↑ K+ uptake
fat
increase triglyceride storage
Clinical use
type I DM
type II DM
life-threatening hyperkalemia
increases intracellular K+
stress-induced hyperglycemia
Toxicity
hypoglycemia
hypersensitivity reaction (very rare)
Insulin Synthesis
first generated as preproinsulin with an A chain and B chain connected by a C peptide.
c-peptide is cleaved from proinsulin after packaging into vesicles leaving behind the A and B chains
Nimesulide
analgesic and antipyretic properties
Nimesulide is a relatively COX-2 selective, non-steroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties. Its approved indications are the treatment of acute pain, the symptomatic treatment of osteoarthritis and primary dysmenorrhoea in adolescents and adults above 12 years old.
Banned - not used
Propofol -Intravenous Anesthetics
- A nonbarbiturate anesthetic
- It is very lipid-soluble, acts rapidly and has a short recovery time.
- It is associated with less nausea and vomiting than some of the other IV anesthetics.
- Propofol is very similar to thiopental in its effects on the cardiorespiratory system.
- It does not have any analgesic properties but lowers the dose of opioid needed when the two agents are used in combination.
- The most significant adverse cardiovascular effect associated with propofol administration is hypotension. It should be used with caution in patients with cardiac disease.
First Generation Cephalosporins
Prototype Drugs are CEFAZOLIN (for IV use) and CEPHALEXIN (oral use).
1. Staph. aureus - excellent activity against b-lactamase-producing strains
Not effective against methicillin-resistant Staph. aureus & epidermidis
2. Streptococci - excellent activity versus Streptococcus sp.
Not effective against penicillin-resistant Strep. pneumoniae
3. Other Gm + bacteria - excellent activity except for Enterococcus sp.
4. Moderate activity against gram negative bacteria.
Caution: resistance may occur in all cases.
Susceptible organisms include:
E. coli
Proteus mirabilis
Indole + Proteus sp. (many strains resistant)
Haemophilus influenzae (some strains resistant)
Neisseria sp. (some gonococci resistant)
Uses
1. Upper respiratory tract infections due to Staph. and Strep.
2. Lower respiratory tract infections due to susceptible bacteria e.g. Strep.pneumoniae in penicillin-allergic patient (previous rash)
3. Uncomplicated urinary tract infections (Cephalexin)
4. Surgical prophylaxis for orthopedic and cardiovascular operations (cefazolin preferred because of longer half-life)
5. Staphylococcal infections of skin and skin structure
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
Antianginal Drugs
Organic Nitrates :
Short acting: Glyceryl trinitrate (Nitroglycerine, GTN), Amyl Nitrate
Long Acting: Isosrbide dinitrate (Short acting by sublingual route), Erythrityl tetranitrate, penta erythrityl tetranitrate
Beta-adrenergic blocking agents : Propanolol, Metoprolol
Calcium channel blockers Verapamil, Nifedipine, Dipyridamole
Mechanism of action
– Decrease myocardial demand
– increase blood supply to the myocardium