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Pharmacology - NEETMDS- courses
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Pharmacology

Heroin (diacetyl morphine)

Heroin is synthetically derived from the natural opioid alkaloid morphine

Largely owing to its very rapid onset of action and very short half-life, heroin is a popular drug of abuse

It is most effective when used intravenously

Heroin is rapidly deacetylated to 6-monoacetyl morphine and morphine, both of which are active at the mu opioid receptor

More lipid soluble than morphine and about 2½ times more potent.  It enters the CNS more readily.

Clotrimazole: Clotrimazole is a potent, specific inhibitor of p450 enzymes.

It is used in some antifungal medications, and in the treatment of yeast infections.

Diphenoxylate (present in Lomotil)

  • A meperidine congener
  • Not absorbed very well at recommended doses.
  • Very useful in the treatment of diarrhea.

Class IV Calcium Channel Blockers
• Block the movement of calcium into conductile and contractile myocardial cells 
• Treatment: treatment of supraventricular tachycardia 
– Diltiazem 
– Verapamil 

Adverse Effects 
• Adverse effects associated with vasodilation of blood vessels throughout the body. 
• CNS – dizziness, weakness, fatigue, depression and headache, 
• GI upset, nausea, and vomiting. 
• Hypotension CHF, shock arrhythmias, and edema 
 

Ibuprofen

used to relieve the symptoms of arthritis, primary dysmenorrhoea, fever; and as an analgesic, especially where there is an inflammatory component.

Indications

rheumatoid arthritis, osteoarthritis, juvenile rheumatoid arthritis, primary dysmenorrhoea

fever, relief of acute and/or chronic pain states in which there is an inflammatory component

MOA

inhibition of  cyclooxygenase (COX); thus inhibiting prostaglandin synthesis.

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)

 

 Adverse reactions to Meperidine

• Generally resemble a combination of opiate and atropine-like effects.

- respiratory depression, - tremors, - delirium and possible convulsions, - dry mouth

• The presentation of mixed symptoms (stupor and convulsions) is quite common in addicts taking large doses of meperidine.

SGLT-2 Inhibitors

canagliflozin
empagliflozin

Mechanism

glucose is reabsorbed in the proximal tubule of the nephron by the sodium-glucose cotransporter 2 (SGLT2)
SGLT2-inhibitors lower serum glucose by increasing urinary glucose excretion
the mechanism of action is independent of insulin secretion or action

Clinical use

type II DM

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