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
CNS acting drugs are of major therapeutic and clinical importance.
They can produce diverse physiologicaland psychologicaleffects such as:
•Induction of Anesthesia
•Relief of Pain
•Prevention of Epileptic seizures
•Reduction of Anxiety
•Treatment of Parkinsonism
•Treatment of Alzheimer's disease
•Treatment of Depression
•Centrally acting drugs also include drugs that are administered without medical intervention like tea, coffee, nicotine, and opiates.
Characteristics of Opioid Receptors
mu1
Agonists : morphine phenylpiperidines
Actions: analgesia bradycardia sedation
mu2
Agonists : morphine phenylpiperidines
Actions: respiratory depression euphoria physical dependence
delta
Actions: analgesia-weak, respiratory depression
kappa
Agonists: ketocyclazocine dynorphin nalbuphine butorphanol
Actions: analgesia-weak respiratory depression sedation
Sigma
Agonists: pentazocine
Action: dysphoria -delerium hallucinations tachycardia hypertension
epsilon:
Agonists: endorphin
Actions: stress response acupuncture
Antiplatelet Drugs:
Whereas the anticoagulant drugs such as Warfarin and Heparin suppress the synthesis or activity of the clotting factors and are used to control venous thromboembolic disorders, the antithrombotic drugs suppress platelet function and are used primarily for arterial thrombotic disease. Platelet plugs form the bulk of arterial thrombi.
Acetylsalicylic acid (Aspirin)
• Inhibits release of ADP by platelets and their aggregation by acetylating the enzymes (cyclooxygenases or COX) of the platelet that synthesize the precursors of Thromboxane A2 that is a labile inducer of platelet aggregation and a potent vasoconstrictor.
• Low dose (160-320 mg) may be more effective in inhibiting Thromboxane A2 than PGI2 which has the opposite effect and is synthesized by the endothelium.
• The effect of aspirin is irreversible.
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.
Treatment modifications to consider if there are concerns regarding vasoconstrictors
- Monitor blood pressure and heart rate preoperatively
- Minimize administration of epinephrine or levonordefrin
- Monitor blood pressure and heart rate 5 min after injection
- May re-administer epinephrine or levonordefrin if blood pressure and heart rate are stable
- Continue to monitor as required
- Consider limiting epinephrine to 0.04 mg, levonordefrin to 0.2 mg
- Avoid epinephrine 1:50,000
- Never use epinephrine-impregnated retraction cord
Chloramphenicol
derived from the bacterium Streptomyces venezuelae
Chloramphenicol is effective against a wide variety of microorganisms, but due to serious side-effects (e.g., damage to the bone marrow, including aplastic anemia) in humans, it is usually reserved for the treatment of serious and life-threatening infections (e.g., typhoid fever). It is used in treatment of cholera, as it destroys the
vibrios and decreases the diarrhoea. It is effective against tetracycline-resistant vibrios.It is also used in eye drops or ointment to treat bacterial conjunctivitis.
Mechanism and Resistance Chloramphenicol stops bacterial growth by binding to the bacterial ribosome (blocking peptidyl transferase) and inhibiting protein synthesis.
Chloramphenicol irreversibly binds to a receptor site on the 50S subunit of the bacterial ribosome, inhibiting peptidyl transferase. This inhibition consequently results in the prevention of amino acid transfer to growing peptide chains, ultimately leading to inhibition of protein formation.
Spectrum of activity: Broad-spectrum
Effect on bacteria: Bacteriostatic