PHM 423 Top 300 Drugs Week 1

Buprenorphine/Naloxone (Suboxone; Zubsolv): Rare but Serious (<1%)

• Stevens-Johnson syndrome

• physical dependence

• tolerance

• elevated liver function tests

• seizures

Buprenorphine/Naloxone (Suboxone; Zubsolv): Drug Class

• Opioid Partial Agonist and Antagonist Combination (C-III)

Buprenorphine/Naloxone (Suboxone; Zubsolv): Uses

• Opioid dependence

Buprenorphine/Naloxone (Suboxone; Zubsolv): MoA

• Buprenorphine: μ-opioid receptor partial agonist, κ-opioid receptor antagonist

• Naloxone: μ-opioid receptor antagonist

Buprenorphine/Naloxone (Suboxone; Zubsolv): Common (>10%)

• Vasodilation

• sweating

• headaches

• insomnia

• constipation

• GI distress

• opioid withdrawal

• dizziness

Buprenorphine/Naloxone (Suboxone; Zubsolv): Dosing (Adults) for Opioid Dependence

• Initial: 2–8 mg sublingually once daily

• may titrate to a maximum of 24 mg/day

Buprenorphine/Naloxone: Brand Name

• Suboxone

• Zubsolv

Buprenorphine/Naloxone (Suboxone; Zubsolv): Key Patient Counseling Points

• Use stool softeners/laxatives for constipation

• Avoid alcohol and CNS depressants

• Place sublingual tablets/films under tongue; do not crush or swallow

• Avoid abrupt discontinuation

Bupropion (Aplenzin, Forfivo XL, Wellbutrin SR, Wellbutrin XL): Rare but Serious (<1%)

• Cardiac dysrhythmia

• mania

• seizure

• suicidal thoughts

• wide QRS complex

Bupropion (Aplenzin, Forfivo XL, Wellbutrin SR, Wellbutrin XL): Drug Class

• Monocyclic Antidepressant

Bupropion (Aplenzin, Forfivo XL, Wellbutrin SR, Wellbutrin XL): Uses

• Depression

• smoking cessation

Bupropion (Aplenzin, Forfivo XL, Wellbutrin SR, Wellbutrin XL): MoA

• Mild dopamine and norepinephrine uptake inhibitor

• no direct effect on serotonin or MAO

Bupropion (Aplenzin, Forfivo XL, Wellbutrin SR, Wellbutrin XL): Common (>10%)

• Agitation

• constipation

• dizziness

• headache

• insomnia

• nausea

• tachyarrhythmia

• tremor

• xerostomia

Bupropion (Aplenzin, Forfivo XL, Wellbutrin SR, Wellbutrin XL): Dosing (Adults) for Depression

• Initial: 150 mg orally daily

• may titrate to max of 450 mg/day

Bupropion: Brand Name

• Aplenzin

• Forfivo XL

• Wellbutrin SR

• Wellbutrin XL

Bupropion (Aplenzin, Forfivo XL, Wellbutrin SR, Wellbutrin XL): Key Patient Counseling Points

• Avoid alcohol and CNS depressants

• Take at the same time daily

• Extended-release tablets may appear intact in stool

Divalproex (Depakote): Rare but Serious (<1%)

• Hepatitis

• palpitation

• pancreatitis

• tachycardia

• thrombocytopenia

• suicidal ideation or behavior

Divalproex (Depakote): Drug Class

• Anticonvulsant

Divalproex (Depakote): Uses

• Seizures (generalized

• complex partial)

• bipolar disorder

• migraine prophylaxis

Divalproex (Depakote): MoA

• Composed of sodium valproate and valproic acid

• increases GABA levels and limits neuronal firing by sodium channel inhibition

Divalproex (Depakote): Common (>10%)

• Abdominal pain

• alopecia

• asthenia

• diarrhea

• diplopia

• dizziness

• headache

• nausea

• somnolence

• tremor

• vomiting

Divalproex (Depakote): Dosing (Adults) for Bipolar Disorder

• Initial: 750 mg orally daily in divided doses

• titrate to 20–30 mg/kg/day (max: 60 mg/kg/day)

Divalproex: Brand Name

• Depakote

Divalproex (Depakote): Key Patient Counseling Points

• Avoid alcohol

• Take with food to prevent GI upset

• Monitor for liver dysfunction (e.g., dark urine, yellow skin)

• Do not discontinue abruptly

Gabapentin (Neurontin, Gralise): Rare but Serious (<1%)

• Stevens-Johnson syndrome

• suicidal thoughts

Gabapentin (Neurontin, Gralise): Drug Class

• Gamma Aminobutyric Acid Analog

• Anticonvulsant

Gabapentin (Neurontin, Gralise): Uses

• Seizures (partial onset)

• postherpetic neuralgia

Gabapentin (Neurontin, Gralise): MoA

• Structurally related to GABA

• exact mechanism unknown

• does not interact with GABA receptors

Gabapentin (Neurontin, Gralise): Common (>10%)

• Dizziness

• somnolence

Gabapentin (Neurontin, Gralise): Dosing (Adults) for Neuralgia

• Initial: 300 mg orally on day 1

• titrate by 300 mg/day increments to maintenance dose of 1800 mg/day

Gabapentin: Brand Name

• Neurontin

• Gralise

Gabapentin (Neurontin, Gralise): Key Patient Counseling Points

• Take first dose at bedtime

• Avoid sudden discontinuation

• Wait 2 hours after antacids

• Avoid activities requiring alertness

Lithium (Lithobid): Rare but Serious (<1%)

• Hypotension

• nephrotoxicity

• seizure

• hypercalcemia

• hyperparathyroidism

Lithium (Lithobid): Drug Class

• Antimanic

Lithium (Lithobid): Uses

• Bipolar disorder (manic episodes and maintenance therapy)

Lithium (Lithobid): MoA

• Alters cation transport, second-messenger systems (e.g., phosphoinositol) inhibited

• influences serotonin/norepinephrine reuptake

Lithium (Lithobid): Common (>10%)

• Cardiac dysrhythmias

• fine tremor

• hypothyroidism

• leukocytosis

• thrombocytosis

• xerostomia

Lithium (Lithobid): Dosing (Adults) for Bipolar Disorder

• Initial: 300 mg orally 2–3 times daily

• titrate to therapeutic levels (maintenance: 900–1200 mg/day in divided doses)

Lithium: Brand Name

• Lithobid

Lithium (Lithobid): Key Patient Counseling Points

• Maintain adequate fluid and normal salt intake

• Report toxicity symptoms (e.g., tremor, ataxia, diarrhea)

• Swallow extended-release tablets whole

• Avoid activities requiring alertness

Naloxone (Narcan): Rare but Serious (<1%)

• Acute withdrawal syndrome

• arrhythmia

• cardiac arrest

• pulmonary edema

• seizures

Naloxone (Narcan): Drug Class

• Opioid Antagonist

Naloxone (Narcan): Uses

• Opioid overdose reversal

Naloxone (Narcan): MoA

• Competes for binding at μ-opioid receptors in the CNS to reverse opioid effects

Naloxone (Narcan): Common (>10%)

• Dizziness

• flushing

• injection site reactions

• nausea

• vomiting

Naloxone (Narcan): Dosing (Adults) for Opioid Overdose

• Initial: 0.4–2 mg intramuscularly, intravenously, or subcutaneously

• may repeat every 2–3 minutes if needed (max 10 mg)

Naloxone: Brand Name

• Narcan

Naloxone (Narcan): Key Patient Counseling Points

• Seek immediate medical attention after use

• Proper administration technique is crucial

• Monitor closely; effects may wear off before opioids are cleared

Nicotine (Nicorette, Nicoderm CQ): Rare but Serious (<1%)

• Bronchospasm

• nicotine overdose

Nicotine (Nicorette, Nicoderm CQ): Drug Class

• Smoking Cessation Aid

Nicotine (Nicorette, Nicoderm CQ): Uses

• Smoking cessation

Nicotine (Nicorette, Nicoderm CQ): MoA

• Stimulates autonomic ganglia, producing feelings of pleasure

• helps prevent withdrawal symptoms during gradual cessation

Nicotine (Nicorette, Nicoderm CQ): Common (>10%)

• Headache

• mouth irritation

• xerostomia

• dyspepsia

• insomnia

Nicotine (Nicorette, Nicoderm CQ): Dosing (Adults) for Smoking Cessation

• Gum: Chew 1 piece every 1–2 hours (max: 24 pieces/day)

• Patch: Apply 1 patch daily

• Lozenge: Use at least 9 lozenges/day

Nicotine: Brand Name

• Nicorette

• Nicoderm CQ

Nicotine (Nicorette, Nicoderm CQ): Key Patient Counseling Points

• Select a quit date

• Chew gum until tingle, then park between cheek and gum

• Rotate patch sites daily

• Avoid eating/drinking before and after gum/lozenge use

Pregabalin (Lyrica): Rare but Serious (<1%)

• Angioedema

Pregabalin (Lyrica): Drug Class

• Analgesic

• Anticonvulsant (C-V)

Pregabalin (Lyrica): Uses

• Neuropathic pain

• fibromyalgia

• partial seizures

• postherpetic neuralgia

Pregabalin (Lyrica): MoA

• GABA analogue

• binds to α₂-delta subunit of voltage-gated calcium channels, reducing calcium-dependent neurotransmitter release

Pregabalin (Lyrica): Common (>10%)

• Dizziness

• somnolence

• ataxia

• headache

• peripheral edema

Pregabalin (Lyrica): Dosing (Adults) for Neuropathic Pain

• Initial: 50 mg orally three times daily

• may titrate to 300 mg/day

Pregabalin: Brand Name

• Lyrica

Pregabalin (Lyrica): Key Patient Counseling Points

• Avoid sudden discontinuation

• Avoid alcohol and CNS depressants

• Use solution within 45 days of opening

• Avoid activities requiring alertness

Sumatriptan (Imitrex, Onzetra, Tosymra, Zembrace): Rare but Serious (<1%)

• Angina

• cardiac dysrhythmia

• coronary arteriosclerosis

• heart block

• hypertension

• myocardial infarction

• stroke

Sumatriptan (Imitrex, Onzetra, Tosymra, Zembrace): Drug Class

• Antimigraine Serotonin Receptor Agonist

Sumatriptan (Imitrex, Onzetra, Tosymra, Zembrace): Uses

• Acute migraine and cluster headaches

Sumatriptan (Imitrex, Onzetra, Tosymra, Zembrace): MoA

• High affinity for serotonin (5-HT) subtypes 1B, 1D, 1F receptors

• vasoconstriction and inhibition of proinflammatory neuropeptides

Sumatriptan (Imitrex, Onzetra, Tosymra, Zembrace): Dosing (Adults) for Migraine

• Initial: 25–100 mg orally once

• max single dose: 100 mg

• may repeat in 2 hours if needed (max: 200 mg/day)

Sumatriptan: Brand Name

• Imitrex

• Onzetra

• Tosymra

• Zembrace

Sumatriptan (Imitrex, Onzetra, Tosymra, Zembrace): Key Patient Counseling Points

• Avoid activities requiring alertness

• Use only for acute migraines

• Report severe cardiovascular symptoms immediately

Topiramate (Topamax): Rare but Serious (<1%)

• Stevens-Johnson syndrome

• erythema multiforme

• metabolic acidosis

• hypohidrosis

• glaucoma

• suicidal ideation

• visual defects

Topiramate (Topamax): Drug Class

• Anticonvulsant

Topiramate (Topamax): Uses

• Seizures

• migraine prophylaxis

Topiramate (Topamax): MoA

• Blocks voltage-dependent sodium channels

• augments GABA activity

• antagonizes AMPA/kainate glutamate receptors

• inhibits carbonic anhydrase

Topiramate (Topamax): Common (>10%)

• Ataxia

• dizziness

• somnolence

• impaired psychomotor performance

• fatigue

• loss of appetite

• nystagmus

• low serum bicarbonate

Topiramate (Topamax): Dosing (Adults) for Migraine Prophylaxis

• Initial: 25 mg orally nightly

• titrate by 25 mg/day weekly (max: 100 mg/day in divided doses)

Topiramate: Brand Name

• Topamax

Topiramate (Topamax): Key Patient Counseling Points

• Avoid alcohol and CNS depressants

• Maintain fluid intake to reduce kidney stone risk

• Avoid hot temperatures

• Do not abruptly discontinue

Varenicline (Chantix): Rare but Serious (<1%)

• Abnormal behavior

• suicidal thoughts

• angioedema

• hypersensitivity reactions

• cardiovascular events

• seizures

• sleepwalking

Varenicline (Chantix): Drug Class

• Smoking Cessation Agent

Varenicline (Chantix): Uses

• Smoking cessation

Varenicline (Chantix): MoA

• Binds to α4β2 nicotinic acetylcholine receptors

• acting as an agonist while preventing nicotine binding

Varenicline (Chantix): Common (>10%)

• Dream disorder

• nausea

• headache

• insomnia

• irritability

Varenicline (Chantix): Dosing (Adults) for Smoking Cessation

• Initial: 0.5 mg orally once daily for 3 days, then 0.5 mg twice daily for 4 days

• increase to 1 mg twice daily

Varenicline: Brand Name

• Chantix

Varenicline (Chantix): Key Patient Counseling Points

• Take after eating with water

• Report mental changes, seizures, or hypersensitivity

• Limit alcohol

• Can combine with other nicotine replacements