A.17 Flashcards
Natural opioids
Morphine,
codeine
opioid receptors
μ, κ, δ
Morphine
MOA: strong μ-OR agonist;
Effect:
1. CNS effect: analgesia, Respiratory depression, Euphoria, Sedation, Miosis, Dysphoria, Antitussive effect, Nausea, Vomiting, Increased muscle rigidity, Epileptogenic.
2. Peripheral effect: ↓BP, Bradycardia, Constipation (↓GI motility), ↑SMC tone, Urinary retention, Bronchoconstriction, Endocrine alterations (↑ACTH, PRL, GH, ADH + ↓LH, FSH);
IND: Analgesia, Strong states of anxiety, Diarrhea, Acute pulmonary edema;
Contra-IND: Head trauma, COPD, Cor pulmonale, Severe hepatic impairment, Alcohol intoxication, Epilepsy;
Extra: metabolized by the liver by CYP2A4, Eliminated via glucoronide conjugation (intermediate compound has much higher activity);
ROA: Morphine sulphate per os 2X30-100mg, Morphine hydrochloride sc. 10-20mg, i.v 1mg - repeated up to 10mg
Morphine
MOA: strong μ-OR agonist;
Effect:
1. CNS effect: analgesia, Respiratory depression, Euphoria, Sedation, Miosis, Dysphoria, Antitussive effect, Nausea, Vomiting, Increased muscle rigidity, Epileptogenic.
2. Peripheral effect: ↓BP, Bradycardia, Constipation (↓GI motility), ↑SMC tone, Urinary retention, Bronchoconstriction, Endocrine alterations (↑ACTH, PRL, GH, ADH + ↓LH, FSH);
IND: Analgesia, Strong states of anxiety, Diarrhea, Acute pulmonary edema;
Contra-IND: Head trauma, COPD, Cor pulmonale, Severe hepatic impairment, Alcohol intoxication, Epilepsy;
Extra: metabolized by the liver by CYP2A4, Eliminated via glucoronide conjugation (intermediate compound has much higher activity);
ROA: Morphine sulphate per os 2X30-100mg, Morphine hydrochloride sc. 10-20mg, i.v 1mg - repeated up to 10mg
Codeine
MOA: Weak μ-OR agonist, centrally acting antitussive (decreased sensibility of cough centers);
Effect: Antitussive, weak analgestic effect in combination with NSAIDs or acetaminophen;
IND: cough;
Extra: Metabolized by CYP2D6, short duration of action
