Fentanyl (Innovar)

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Name: Fentanyl (Innovar)

Class: Opioid (Synthetic-Analgesic)

Mechanism: Agonist of opioid receptors. Causes analgesia (­ threshold for pain, ¯ subjective rxn), antitussive effects, euphoria/dysphoria (atypical), sedation (rarely stimulation), resp. depression, miosis, n/v, ¯ body temp., ­ ACTH/PRO/GH, ¯ LH/TSH (hormone effects usu. non-consequential), occasionally hypotension, constipation, ­ biliary/ureteral/bladder muscle tone, ¯ uteral muscle tone, histamine release (hypotension, urticaria, itching).

Absorption: Parenteral, transdermal patch, lollipop.

Metabolism.: Hepatic conjug. ® polar Metabolismolites.

Excretion, : Urine. Duration of analgesia—1-1.5 hr.

Toxicity/S.E.s: Histamine release ® asthma in suscept. patients. Use w/caution w/compromised resp. patients. CO2 retention ® ­ intracranial pressure (may mask signs of head injury). Poisoning ® coma, severe resp. depression, pinpoint pupils. Rapid onset of tolerance (up to 100x) to analgesia, euphoria/dysphoria, sedation, n/v, resp. depression, cough suppression. Physical dependence—abrupt w/drawal ® rhinorrhea, lacrimation, chills, goose pimples, hyperventilation, mydriasis, myalgia, vomiting, diarrhea, anxiety, hostility (but it’s not fatal). Also psychological dependence. Drug interactions—sedative hypnotics ® severe CNS/resp. depression; phenothiazines/tricyclic antidepressants ® ­ sedation, freq. resp. depression.

Utility: Analgesia. Induction of general anesthesia.

Special Features: Very high maximum efficacy. High addiction/abuse liability. Psych. dependence.

 

Pentazocine (Talwin)

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Name: Pentazocine (Talwin)

Class: Opioid (Synthetic-Analgesic)

Mechanism: Mixed agonist-antagonist of opioid receptors. Causes analgesia (­ threshold for pain, ¯ subjective rxn), sedation, resp. depression.

Absorption: IM, subcut, oral (1st pass Metabolism ® med. oral:parenteral potency).

Metabolism.: Hepatic conjug.®polar Metabolismolites. Excretion, : Urine. Duration of analgesia—3-4 hr.

Toxicity/S.E.s: CO2 retention ® ­ intracranial pressure (may mask signs of head injury). Tolerance (up to 100x) to analgesia, sedation, resp. depression. Physical dependence—abrupt w/drawal ® rhinorrhea, lacrimation, chills, goose pimples, hyperventilation, mydriasis, myalgia, vomiting, diarrhea, anxiety, hostility (but it’s not fatal). Also psychological dependence. Precipitates w/drawal synd. Large doses ® dysphoria & hallucinations. Drug interactions—sedative hypnotics ® severe CNS/resp. depression; phenothiazines/tricyclic antidepressants ® ­ sedation, freq. resp. depression.

Utility: Analgesia. Orig. thought to lack abuse liability.

Special Features: Mod. maximum efficacy. Low addiction/abuse liability. Psych. dependence.

 

Propoxyphene (Darvon)

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Name: Propoxyphene (Darvon)

Class: Opioid (Synthetic-Analgesic)

Mechanism: Agonist of opioid receptors. Causes analgesia (­ threshold for pain, ¯ subjective rxn), antitussive effects, euphoria/dysphoria (atypical), sedation (rarely stimulation), resp. depression, miosis, n/v, ¯ body temp., ­ ACTH/PRO/GH, ¯ LH/TSH (hormone effects usu. non-consequential), occasionally hypotension, constipation, ­ biliary/ureteral/bladder muscle tone, ¯ uteral muscle tone, histamine release (hypotension, urticaria, itching).

Absorption: Oral

Metabolism.: Hepatic conjug. ® polar Metabolismolites.

Excretion, : Urine. Duration of analgesia—4-5 hr.

Toxicity/S.E.s: Histamine release ® asthma in suscept. patients. Use w/caution w/compromised resp. patients. CO2 retention ® ­ intracranial pressure (may mask signs of head injury). Poisoning ® coma, severe resp. depression, pinpoint pupils. Rapid onset of tolerance (up to 100x) to analgesia, euphoria/dysphoria, sedation, n/v, resp. depression, cough suppression. Physical dependence—abrupt w/drawal ® rhinorrhea, lacrimation, chills, goose pimples, hyperventilation, mydriasis, myalgia, vomiting, diarrhea, anxiety, hostility (but it’s not fatal). Also psychological dependence. Drug interactions—sedative hypnotics ® severe CNS/resp. depression; phenothiazines/tricyclic antidepressants ® ­ sedation, freq. resp. depression.

Utility: Limited analgesia (no more than aspirin in usu. therapeutic dose, but augments the effects of aspirin & acetaminophen.

Special Features: Very low maximum efficacy (limited analgesia). Low addiction/abuse liability.

 

Meperidine (Demerol)

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Name: Meperidine (Demerol)

Class: Opioid (Synthetic-Analgesic)

Mechanism: Agonist of opioid receptors. Causes analgesia (­ threshold for pain, ¯ subjective rxn), antitussive effects, euphoria/dysphoria (atypical), sedation (rarely stimulation), resp. depression, miosis, n/v, ¯ body temp., ­ ACTH/PRO/GH, ¯ LH/TSH (hormone effects usu. non-consequential), occasionally hypotension, constipation, ­ biliary/ureteral/bladder muscle tone, ¯ uteral muscle tone, histamine release (hypotension, urticaria, itching).

Absorp.: IM, subcut., oral (1st pass Metabolism ® med. oral:parenteral potency).

Metabolism.: Hepatic conjug.®polar Metabolismolites. Excretion, : Urine. Duration of analgesia—2-4 hr.

Toxicity/S.E.s: Histamine release ® asthma in suscept. patients. Use w/caution w/compromised resp. patients. CO2 retention ® ­ intracranial pressure (may mask signs of head injury). Poisoning ® coma, severe resp. depression, pinpoint pupils. Rapid onset of tolerance (up to 100x) to analgesia, euphoria/dysphoria, sedation, n/v, resp. depression, cough suppression. Physical dependence—abrupt w/drawal ® rhinorrhea, lacrimation, chills, goose pimples, hyperventilation, mydriasis, myalgia, vomiting, diarrhea, anxiety, hostility (but it’s not fatal). Also psychological dependence. Drug interactions—sedative hypnotics ® severe CNS/resp. depression; phenothiazines/tricyclic antidepressants ® ­ sedation, freq. resp. depression; MAO inhib ® hyperpyrexia, coma, convulsions.

Utility: Analgesia.

Special Features: High maximum efficacy. High addiction/abuse liability. Psych. dependence.Less severe constipation, effect on smooth muscle. Less predictable miosis.

 

Methadone (Dolophine)

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Name: Methadone (Dolophine)

Class: Opioid (Synthetic-Analgesic) (Withdrawal Suppressant)

Mechanism: Agonist of opioid receptors. Causes analgesia (­ threshold for pain, ¯ subjective rxn), antitussive effects, euphoria/dysphoria (atypical), sedation (rarely stimulation), resp. depression, miosis, n/v, ¯ body temp., ­ ACTH/PRO/GH, ¯ LH/TSH (hormone effects usu. non-consequential), occasionally hypotension, constipation, ­ biliary/ureteral/bladder muscle tone, ¯ uteral muscle tone, histamine release (hypotension, urticaria, itching).

Absorption: IM, subcut., oral (high oral:parenteral potency).

Metabolism.: Hepatic conjug. ® polar Metabolismolites.

Excretion, : Urine. Duration of analgesia—4-6 hr.

Toxicity/S.E.s: Histamine release ® asthma in suscept. patients. Use w/caution w/compromised resp. patients. CO2 retention ® ­ intracranial pressure (may mask signs of head injury). Poisoning ® coma, severe resp. depression, pinpoint pupils. Rapid onset of tolerance (up to 100x) to analgesia, euphoria/dysphoria, sedation, n/v, resp. depression, cough suppression. Physical dependence—abrupt w/drawal ® rhinorrhea, lacrimation, chills, goose pimples, hyperventilation, mydriasis, myalgia, vomiting, diarrhea, anxiety, hostility (but it’s not fatal). Also psychological dependence. Drug interactions—sedative hypnotics ® severe CNS/resp. depression; phenothiazines/tricyclic antidepressants ® ­ sedation, freq. resp. depression.

Utility: Treatment of physical dependence to other opioids, esp. heroin (less severe w/drawal synd.). Analgesia. Migraine relief.

Special Features: High maximum efficacy. High addiction/abuse liability. Psych. dependence.