NEET MDS Lessons
Pharmacology
Osmotic diuretics
An osmotic diuretic is a type of diuretic that inhibits reabsorption of water and sodium. They are pharmacologically inert substances that are given intravenously. They increase the osmolarity of blood and renal filtrate.
Mechanism(s) of Action
1. Reduce tissue fluid (edema)
2. Reflex cardiovascular effect by osmotic retention of fluid within vascular space which increases blood volume (contraindicated with Congestive heart failure)
3. Diuretic effect
o Makes H2O reabsorption far more difficult for tubular segments insufficient Na & H2O capacity in distal segments
o Increased intramedullary blood flow (washout)
o Incomplete sodium recapture (asc. loop). this is indirect inhibition of Na reabsorption (Na stays in tubule because water stays)
o Net diuretic effect:
Tubular concentration of sodium decreases
Total amount of sodium lost amount increases
GFR unchanged or slightly increased
Toxicity
Circulatory overload, dilutional hyponatremia, Hyperkalemia, edema, skin necrosis
Agents
Mannitol
Miconazole
Miconazole is an imidazole antifungal agent commonly used in topical sprays, creams and ointments applied to the skin to cure fungal infections such as Athlete's foot and Jock itch. It may also be used internally to treat vaginal yeast infection.
When used by a person taking the anticoagulant medication warfarin, Miconazole may cause an adverse reaction which can lead to excessive bleeding or bruising.
Propoxyphene
- A methadone analog.Used orally to relieve mild to moderate pain.
- A typical opiate, it does not possess anti-inflammatory or antipyretic actions, but has little or no antitussive activity.
- Cannot be used parenterally because of irritant properties.
- Has a low addiction potential primarily due to its lack of potency as an opiate.
- The most common adverse side effects are:• dizziness, drowsiness, and nausea and vomiting. • these effects are more prominent in ambulatory patients.
- Withdrawal symptoms have occurred in both adults and in neonates following use of the drug by the mother during pregnancy.
- CNS depression is additive with other CNS depressants.
Procaine penicillin Procaine penicillin is a combination of benzylpenicillin with the local anaesthetic agent procaine. This combination is aimed at reducing the pain and discomfort associated with a large intramuscular injection of penicillin.
Indications
respiratory tract infections where compliance with oral treatment is unlikely ,syphilis, cellulitis
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
Hypothalamic - Pituitary Drugs
Somatropin
Growth hormone (GH) mimetic
Mechanism
agonist at GH receptors
increases production of insulin growth factor-1 (IGF-1)
Clinical use
GH deficiency
increase adult height for children with conditions associated with short stature
Turner syndrome
wasting in HIV infection
short bowel syndrome
Toxicity
scoliosis
edema
gynecomastia
increased CYP450 activity
Octreotide
Somatostatin mimetic
Mechanism
agonist at somatostatin receptors
Clinical use
acromegaly
carcinoid
gastrinoma
glucagonoma
acute esophageal variceal bleed
Toxicity
GI upset
gallstones
bradycardia
Oxytocin
Mechanism
agonist at oxytocin receptor
Clinical use
stimulation of labor
uterine contractions
control of uterine hemorrhage after delivery
stimulate milk letdown
Toxicity
fetal distress
abruptio placentae
uterine rupture
Desmopressin
ADH (vasopressin) mimetic
Mechanism
agonist at vasopressin V2 receptors
Clinical use
central (pituitary) diabetes insipidus
hemophilia A (factor VIII deficiency)
increases availability of factor VIII
von Willebrand disease
increases release of von Willebrand factor from endothelial cells
Toxicity
GI upset
headache
hyponatremia
allergic reaction
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).