amitriptyline (Elavil, Merck) – [tabs 10, 25, 50, 75, 100, 150 mg] Indic/Dosage: depression: 50-150 mg qhs (for elderly 10 mg tid and 20 mg qhs may be sufficient; reduce dose for hepatic impairment); off-label for neuropathic pain (start at doses lower than for depression); Action: tertiary amine tricyclic, NE/seratonin reuptake inhibitor; also has anti α1-adrenergic and potent antimuscarinic properties; Contra: acute post-MI, concomitant MAOI use; Warn/Prec: CV disorders (can cause HTN), hyperthyroidism, schizophrenia/paranoia, pregnancy D, discontinue before elective surgery; withdraw gradually after long-term use to avoid insomnia and abdominal discomfort; black box warning for increased risk of suicidality in< 25 years old; Adverse Rxs: dry mouth^*, blurred vision^*, constipation^*, urinary retention^*, cardiovascular effects (tachycardia^*, prolongation of AV conduction), drug fever, leukopenia, weight gain, somnolence, seizures, photosensitivity, rash, abdominal distress, gynecomastia, testicular swelling, menstrual irregularity, sexual dysfunction; Monitoring: baseline and periodic leukocyte and differential counts, LFTs, ECG; pts with cardiovascular issues require surveillance.

desipramine (Norpramin, Sanofi-Aventis) – [tabs 10, 25, 50, 75, 100, and 150 mg] Indic/Dosage: depression; off-label use includes treatment of neuropathic pain and ADHD. Start 25-100 mg qday or in divided doses. Usual effective dose is 100-200 mg/d, max 300 mg/d. Action: primarily inhibits norepinephrine reuptake; Contra: In the acute recovery phase after MI, concomitant MAOI use; Adverse Rxs: blurred vision, constipation, drowsiness, dry mouth or hypotension; Monitoring: pts with hx of cardiovascular disease require closer surveillance. Black box warning for increased risk of suicidality in those < 25 years old.

duloxetine (Cymbalta, Eli Lilly) – [delayed-release caps 20, 30, 60 mg] Indic/Dosage: FDA-approved for depression (40-60 mg daily) and in 2003 for diabetic peripheral neuropathy; Action: selective serotonin and norepinephrine reuptake inhibitor; Contra: end-stage renal disease (requiring dialysis) or in severe renal impairment (estimated CrCl <30 mL/min); Warn/Prec: CV disorders (can cause HTN), hyperthyroidism, schizophrenia/paranoia, pregnancy C, d/c before elective surgery; withdraw gradually after long-term use to avoid insomnia and abdominal discomfort, drug interactions (with TCAs, phenothiazines, and type 1C antiarrhythmics) black box warning for increased risk of suicidality in those < 25 years old; Adverse Rxs: nausea^*, somnolence^*, dry mouth^*, urinary hesitancy; Monitoring: BP and HR, check efficacy after 12 weeks, observe coexisting depression/bipolar disorder for suicide risk or mania/hypomania.

milnacipran (Savella, Cypress Bioscience) – [tabs 12.5, 25, 50, 100 mg] Indic/Dosage: FDA-approved for fibromyalgia; Off-label use for depression. Dosing should be titrated according to the following schedule: Day 1: 12.5 mg once, Days 2-3: 25 mg/day (12.5 mg twice daily), Days 4-7: 50 mg/day (25 mg twice daily), After Day 7: 100 mg/day (50 mg twice daily). Daily maximum 200 mg/day; Action: serotonin and norepinephrine reuptake inhibitor. Warn/Prec: Not approved for pediatric patients. Black box warning for increased risk
of suicidality in those < 25 years old, coadministration with a monoamine oxidase inhibitor (MAOI) or use within 14 days of initiating or discontinuing therapy with an MAOI is not recommended; caution in patients with hepatic and renal dysfunction; pregnancy C; Adverse Rxs: nausea^*, palpitations^*; dry mouth; headache; constipation; hyperhydrosis, vomiting, dizziness. Monitoring: BP and HR, depressive sx and suicide risk; withdrawal sx when discontinued; serotonin syndrome or neuroleptic malignant syndrome (NMS)-like reactions.

mirtazapine (Remeron, Organon) – [tabs 15, 30, 45 mg; orally disintegrating (SolTab) 15, 30, 45 mg] Indic/Dosage: FDA-approved for depression; Off-label use for anxiety and neuropathic pain; start 15 mg po qhs, titrate up to q 1-2 weeks to 45 mg/d; Action:Enhances central serotonergic and noradrenergic activity via activity as antagonist central presynaptic α2 adrenergic receptor; potent 5-HT2 and 5-HT3 receptor angatonist; potent histamine H1-receptor antagonist; moderate alpha-1 adrenergic antagonist; moderate muscarinic receptor antagonist; metabolized via CYP2D6 and 1As; Warn/Prec: Blackbox warning for increased risk of suicidality in children, adolescents and young adults; coadministration with a monoamine oxidase inhibitor (MAOI) or use within 14 days of initiating or discontinuing therapy with an MAOI is not recommended; caution in patients with hepatic and renal dysfunction; avoid Sol Tab in phenylketonurics (contains phenylalanine); pregnancy C; Adverse Rxs: Somnolence^*, dizziness^*, asthenia^*, increased appetite/weight gain^*, dry mouth^*, constipation, nausea, hypercholesterolemia, ALT (SGPT) elevation, activation of hypomania/mania, seizure, rare agranulocytosis.

nortriptyline (Palemor, Mallinckrodt; Aventyl, Ranbaxy) – [caps 10, 25, 50, 75 mg. Oral solution 10 mg/5 ml] Indic/Dosage: depression; off-label use includes chronic pain modification (including temporomandibular joint disorder) and prevention of migraines. Start 25 mg qhs or divided bid-qid. Usual effective dose is 75-100 mg/d, max 150 mg/d. Action: primarily inhibits norepinephrine reuptake, and to a lesser extent serotonin; Contra: In the acute recovery phase after MI, concomitant MAOI use; Adverse Rxs: dry mouth, drowsiness, orthostatic hypotension, urinary retention, constipation, irregular heartbeat, and sexual dysfunction; Monitoring: pts with hx of cardiovascular disease, stroke, glaucoma, and/or seizures require closer surveillance. Obtain EKG at baseline and monitor for QT prolongation.

venlafaxine (Effexor, Pfizer) – [caps, extended release (Effexor XR) 37.5, 75, 150 mg; tabs 25, 37.5, 50, 75, 100 mg] Indic/Dosage: FDA-approved for depression, generalized anxiety disorder, social anxiety disorder and panic disorder; off-label use for neuropathic pain and migraine prophylaxis; start 25 mg po tid (or 75 mg/d if using Effexor XR), titrate every 4 days up to 225 mg/d; Action: selective serotonin and norepinephrine reuptake inhibitor; metabolized via CYP2D6; Warn/Prec: Blackbox warning for increased risk of suicidality in children, adolescents, and young adults; avoid co-administration with MAOI; avoid starting venlafaxine within 14 days of discontinuing MAOI; avoid starting MAOI until at least 7 days after discontinuing venlafaxine; monitor for serotonin syndrome if using venlafaxine together with SNRI, SSRI or triptans; may cause hypertension; may cause mydriasis, hence monitor those at risk for narrow-angle glaucoma; may lead to hyponatremia, bleeding; hypercholesterolemia, interstitial lung disease, eosinophilic pneumonia; pregnancy C; Adverse Rxs: abnormal ejaculation^*, anorgasmia^*, impotence^*, somnolence^*, dry mouth^*, sweating^*, nausea^*, decreased libido^*, abnormal dreams, nervousness, pharyngitis, constipation, flatulence, insomnia, tremor, abnormal vision, hypertension,
vasodilation, yawning, anorexia; Monitoring: BP and HR; check for mania/hypomania; check efficacy after 12 weeks; monitor height and weight in pediatric patients; desvenlafaxine (Pristiq, Pfizer – [extended release tabs 50, 100 mg]) is metabolite of venlafaxine and is FDA-approved for major depressive disorder. Taken qd.

baclofen (Lioresal, Novartis) – [tabs 10, 20 mg; intrathecal] Indic/Dosage: spasticity: titrate to max dose of 20 mg qid as follows: 5 mg tid × 3d, then 10 mg tid × 3d, then 15 mg tid × 3d, then 20 mg tid × 3d, increase as needed; consider intrathetcal (IT) pump if oral route is effective but titration is limited by side-effects; no indication of oral form for spasticity due to stroke, Parkinson’s disease, or cerebral palsy; Action: analog of γ-aminobutyric acid thought to bind to GABA-B receptors, inhibiting Ca influx into presynaptic terminals and suppressing spinal cord excitatory neurotransmitters; Warn/Prec: impaired renal fxn, risk of seizure if withdrawn too quickly (therefore, should taper off over approximately 1wk or so), pregnancy C; Adverse Rxs (oral baclofen): drowsiness^*, dizziness^*, headache^*, N/V^*, lassitude^*, GI upset^*, urinary frequency, confusion, CNS depression, slurred speech, seizures, blurred vision, nasal congestion, weakness, hypotonia, HTN, CV collapse, respiratory failure, pruritus, rash, increased LFTs; (IT baclofen): fatigue^*, drowsiness^*; Overdosage: IV physostigmine 1-2 mg.

clonidine (Catapres, Boehringer Ingelheim) – [tabs 0.1, 0.2, 0.3 mg; TTS qwk patch 0.1/24, 0.2/24, 0.3 mg/24 hr] Indic/Dosage: HTN: start orally at 0.1-0.3 mg bid, or TTS 0.1 mg/24 hr qwk, maximum dose is 2.4 mg/d orally or TTS 0.3 mg/24 hr qwk; off label for spasticity: dosing similar to HTN; IT clonidine used investigationally for spasticity and neuropathic pain; Action: central α-adrenergic agonist that ↓ sympathetic discharge; Warn/Prec: CV disease, impaired liver/renal fxn, withdraw gradually to avoid rebound HTN, pregnancy C; Adverse Rxs: dry mouth/eyes, h/a, dizziness, nausea, constipation, sedation, weakness, fatigue, orthostatic hypotension, edema, anorexia, erectile dysfunction, joint pain, leg cramps.

cyclobenzaprine (Flexeril, McNeil) – [tabs 5, 10 mg] Indic/Dosage: muscle spasm due to acute painful musculoskeletal conditions: 10 mg tid, max 60 mg/d, not to exceed 2-3 wks; Action

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