Morphine (MS, Contin)

Classification

Pharmacokinetics

Pharmacodynamics

Adverse effects

Safety

Developmental concerns

Legal & ethical issues

Genetics and meds

Classification: Opioid

Pharmacokinetics: IV, onset 5-10 min, Peak 20min, duration 4 hrs, Large 1st pass effect.  All routes: IV, IM, intrathecal, epidural, po, rectal

Pharmacodynamics: Binds to opioid receptors

Adverse effects: Respiratory depression, pruritis, n/v, constipation, dyspnea

Safety: Monitor respiratory status, rate and O2 sat.  Black box warnings, Usual IV dose: 2-10mg q4h, doses vary w/ route.

Developmental concerns: Elderly > risk for AE. Pregnancy =category C.  Peds intermittent dosing 0.03-0.1 mg/kg/dose

Legal & ethical issues: Schedule 2, pain relief vs. risk for dependence/abuse

Genetics and meds: some evidence of genetic variability affecting response

Fentanyl (Duragesic)

Classification: Opioid (synthetic)

Pharmacokinetics: IV, transdermal, SL, buccal, mucous membrane, nasal, epidural and IM.  IV: onset <1 min, Peak 3-5min, duration 1/2-1hr, protein bound 80%, routes: SL, transdermal, buccal, mucous membranes, nasal, IV, IM, epidural

Pharmacodynamics: Binds to opioid receptors

AE: Apnea, laryngospasm, muscle rigidity, respiratory depression, constipation, dyspnea, hypoxia, n/v, pruritis

Safety: Pregnancy = category C, high risk for resp depression, 50-100mcg q1-2h, txdermal patches -disposal (label, cut into pieces, slower onset), remove old patches when applying new, IV admin too fast = > muscle rigidity

Developmental Concerns: elderly > confusion, Peds 1-5 mcg/kg/hr

Legal & ethical: Schedule 2

Genetics and meds: some evidence of genetic variability affects response

Classification: Opioid

Pharmacokinetics: PO, fast onset, peak 60-90min, duration 3-6hrs. PO, rectal.

Pharmacodynamics: Binds to opiate receptors

AE: Respiratory depression, confusion, dizziness, constipation

Safety: Monitor respiration.  Assess BP and pulse before and during.  Usual PO dose 5-10mg q3-4h

Developmental: Peds 0.05-0.15mg/kg q4h, crosses placenta + breast milk.  Pregnancy =category B

Legal & ethical: Schedule 2

Classification: Opioid antagonist

Pharmacokinetics: IV, IM, subq.  IV: fast onset, unknown peak, duration 45 minute.  Liver metabolism.

Pharmacodynamics: Blocks opioid receptors from opioids.  Reverses CNS and respiratory depression.

AE: Ventricular arrhythmias

Safety: 0.02-0.2mg q2-3min until response.  Repeat 1-2h PRN. Peds: 0.01mg/kg q2-3min until response. Pregnancy category B.

Developmental concerns:

Legal & ethical issues

Genetics and meds

Classification: antipyretic, analgesic

Pharmacokinetics: IV,PO, rectal. IV: onset medium, peak 1-3hrs, duration 3-8hrs.

Pharmacodynamics: Inhibits prostaglandins

AE: Hepatoxicity, AGEP, Steven Johnson synd., toxic epidermal necrolysis.

Safety: crosses placenta and gets in breast milk. Pregnancy: cat B (oral/rectal) C (IV). PO: 325-650mg q6h. IV: 1000mg q6h. Peds: 15mg/kg q6h

Developmental concerns

Legal & ethical issues

Genetics and meds

Classification: anesthetic (local), antiarrhythmic (IV/IM)

Pharmacokinetics: Lipid soluble. IV: onset and peak immediate, duration 10-20min. Local: rapid onset, peak unknown, duration 1-3hr.

Pharmacodynamics: Suppresses ventrical depolarization.  Inhibits ion txport preventing nerve impulse.

AE: Seizure, confusion, drowsiness, MI, stinging, anaphylaxis

Safety: Pregnancy cat B, Local: 2-3 times qd.  IV: 1-1.5mg/kg bolus, 0.5-0.7mg/kg q5-10min up to3mg/kg total, then infuse 1-4mg qmin.

Developmental concerns: caution in elderly. Peds: 1 mg/kg bolus, 20-50 mcg/kg/min cont. infusion.

Legal & ethical issues

Genetics and meds

Classification: General anesthetic

Pharmacokinetics: IV only, lipid soluble, rapid onset, unknown peak, duration 3-5 min.

Pharmacodynamics: Unknown. Hypnotic and amnesic, no analgesia

AE: Apnea, bradycardia, hypotension, burnging, stinging, pain, propofol infusion syndrome

Safety: 40mg q10min until induction, 100-200 mcg/kg/min.

Developmental concerns: Peds: 2.5-3.5 mg/kg, 125-300 mcg/kg/min

Legal & ethical issues: CNS and respiratory depression w/ opioid, alcohol, antihistamines, sedative/hypnotics.

Genetics and meds

Classification: Antianxiety, sedative/hypnotic, benzodiazepine

Pharmacokinetics: IN,IV, IM. Big 1st pass effect.  IV: onset fast, peak rapid, duration 2-6h

Pharmacodynamics: CNS depression

AE: Apnea, laryngospasm, respiratory depression, MI, phlebitis

Safety: Schedul 4, pregnancy cat D.  0.01-0.05 mg/kg q10-15min. 0.02-0.1 mg/kg/hr.

Developmental concerns: Reduced dose in geri.

Legal & ethical issues

Genetics and meds

Prochlorperazine (Compazine)

Classification: Antiemetic/antidopaminergic

Pharmacokinetics:PO, rectal, IM, IV.  Lipid soluble.  IV onset: rapid, peak 10-30min, duration 3-4h.

Pharmacodynamics: Alters dopamine effect in CNS, depresses CTZ

AE: Neuroleptic malignant synd., extrapyrimidal rxns, blurred vision, dry eyes, dry mouth, constipation

Safety: Pregnancy cat C, 2.5-10mg

Developmental concerns: Caution in lactation, decreased geri dose

Legal & ethical issues

Genetics and meds

Classification: antiemetic, antihistamine, sedative/hypnotic

Pharmacokinetics:PO, rectal, IM, IV.  Lipid soluble. IV onset 2-5min, peak unknown, duration 4-12 hr

Pharmacodynamics: Inhibits CTZ, blocks histamine

AE: Neuroleptic malignant syndrome, confusion, disorientation, sedation

Safety: 12.5-25 mg q4h PRN

Developmental concerns: Can cause fatal respiratory despression in peds. Peds 0.25-1 mg/kg q4-6h

Legal & ethical issues

Genetics and meds

Classification: Antiemetic

Pharmacokinetics: IM, PO, IV: onset rapid, peak 15-30min, duration 4-8hrs.

Pharmacodynamics: Blocks serotonin at 5-HT3 receptors in vagal nerve and CTZ

AE: Torsades de Pointes, headache, constipation, diarrhea, hepatic toxicity

Safety:0.15 mg/kg (max=16mg) Do not use with apomorphine.

Developmental concerns: Peds 0.15 mg/kg

Legal & ethical issues

Genetics and meds

Classification: Antiemetic (off label hiccups)

Pharmacokinetics: Lipid soluble, PO, IM, IV: onset fast, peak immediate, duration unknown.

Pharmacodynamics: Blocks dopamine receptors in CTZ

AE: Neuroleptic malignant synd., drowsiness, extrapyrimidal rxns., restlessness

Safety:

Developmental concerns:

Legal & ethical issues

Genetics and meds