Pharmacology Mnemonics - Flash Cards

Name: Diphenoxylate-Atropine (Lomotil)

Class: Opioid (Antidiarrheal)

Mechanism: Increased gastric tone ® delayed gastric emptying. ­ tone and ¯ propulsive peristaltic waves in large intest. ® ¯ gut motility. Effects due to inhib. of ACh release by neurons in the intest. wall. Naloxone sensitive.

Absorption: Oral

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Recommended dose ® dizziness, drowsiness, mild euphoria. Excessive doses ® pronounced euphoria, potentially serious respiratory depression (may not be evident until 12-30 hr later). ¯ peristalsis ® ¯ evacuation of bacteria and toxins. Use w/great caution in kids. Potentiates effects of barbiturate, tranquilizers, alcohol, other narcotics. Hypertensive crisis w/MAOI.

Utility: Antidiarrheal.

Special Features:

Name: Loperamide (Imodium)

Class: Opioid (Antidiarrheal) (OTC)

Mechanism: Increased gastric tone ® delayed gastric emptying. Increase tone and decreasesd propulsive peristaltic waves in large intest. ® decreased gut motility. Effects due to inhib. of ACh release by neurons in the intest. wall. Naloxone sensitive. Anti-secretory effect (non-naloxone sensitive).

Absorption: Oral

Dist.: 90% ® GI tract and liver. Very little CNS.

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: ¯ peristalsis ® ¯ evacuation of bacteria and toxins.

Utility: Antidiarrheal.

Special Features: No abuse liability. Preferred anti-diarrheal of the opioids. Less potential for analgesia, respiratory depression, and addiction than other opioids. Much safer than other opioids. Longer lasting effects than dephnoxylate.

Name: Tramadol (Ultram)

Class: Opioid (Synthetic-Analgesic)

Mech: Low affinity binding of tramadol to mu-opioid receptors and higher affinity binding of the M1 Metabolismolite. Opioid effects only partially antagonized by naloxone. Also inhibits reuptake of norepinephrine and serotonin.

Absorption:

Metabolism:

Excretion, t½:

Toxicity/S.E.s: Sim. to opioids—dizziness, somnolence, nausea, constipation, sweating, & pruritus. Unlike opioids, significantly less respiratory depression, no histamine release. At therapeutic doses, no effect on heart rate, left-ventricular function, or cardiac index. Some orthostatic hypotension. Seizures. Use w/caution w/CNS depressants, MAO inhibitors. May trigger opioid w/drawal symptoms.

Utility: Analgesia.

Special Features: Inhib. reuptake of NE and 5HT.

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, t½: 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.

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, t½: 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.

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, t½: 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.

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, t½: 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.

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, t½: 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.

Name: Dextromethorphan

Class: Opioid (Semi-synthetic) (OTC)

Mechanism: Agonist of opioid receptors ® depression of CNS cough center.

Absorption: Oral.

Metabolism.: Hepatic conjug. ® polar Metabolismolites.

Excretion, t½: Urine.

Toxicity/S.E.s:High doses ® hallucinations. Potentially fatal interactions with MAOIs.

Utility: Antitussant.

Special Features: Minimal addiction/abuse liability.

Name: Heroin

Class: Opioid (Semi-synthetic)

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). Init. ¯ of adenylate cyclase in locus coeruleus & symp. pregang. neurons. Tolerance develops.

Absorption: IM, subcut., mucous membranes, oral, smoking.

Metabolism.: Hepatic conjug. ® polar Metabolismolites. Excretion, t½: Urine.

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 (prob. med. by hyperactive adenylate cyclase) ® 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.

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

Name: Codeine

Class: Opioid (Alkaloid)

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., mucous membranes, oral (high oral:parenteral potency).

Metabolism.: Hepatic conjug. ® polar Metabolismolites.

Excretion, t½: Urine. Duration of analgesia—3-4 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.

Utility: Antitussant. Analgesia.

Name: Morphine

Class: Opioid (Alkaloid)

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., mucous membranes, intrathecal, oral (1st pass Metabolism ® low oral:parenteral potency)

Metabolism.: Hepatic conjug. ® polar Metabolismolites.

Excretion, t½: 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: Analgesia. Intrathecal for post-surg. pain ® long duration of action, few side effects.

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