CNS Drugs
atomoxetine
Trade name: Strattera Pharmacological Class: Norepinephrine Reuptake Inhibitor with Anti-ADHD Effects Mechanism of Action: Selectively inhibits the reuptake of norepinephrine (Ki 4.5nM) with little to no activity at the other neuronal reuptake pumps or receptor sites. Physiological Effects: Therapeutic Uses: Treatment of attention deficit/hyperactivity disorder (ADHD)
hydroxyzine
Trade name: Vistaril, Atarax Pharmacological Class: Mechanism of Action: Physiological Effects: Therapeutic Uses:
methylphenidate
Trade name: CONCERTA, Ritalin Pharmacological Class: Methylphenidate Mechanism of Action: Mild CNS stimulant; blocks the reuptake of norepinephrine and dopamine into presynaptic neurons; appears to stimulate the cerebral cortex and subcortical structures similar to amphetamines Physiological Effects: Therapeutic Uses: Treatment of attention-deficit/hyperactivity disorder (ADHD); symptomatic management of narcolepsy (except Concerta®, Daytrana®, Metadate CD®, Ritalin LA®, and Quillivant™ XR)
lidocaine
Trade name: Pharmacological Class: Amide-type Local Anesthetic (Sodium Channel Blocker) Mechanism of Action: Class Ib antiarrhythmic; suppresses automaticity of conduction tissue, by increasing electrical stimulation threshold of ventricle, His-Purkinje system, and spontaneous depolarization of the ventricles during diastole by a direct action on the tissues; blocks both the initiation and conduction of nerve impulses by decreasing the neuronal membrane's permeability to sodium ions, which results in inhibition of depolarization with resultant blockade of conduction Physiological Effects: Therapeutic Uses: Local and regional anesthesia by infiltration, nerve block, epidural, or spinal techniques; acute treatment of ventricular arrhythmias from myocardial infarction or cardiac manipulation (eg, cardiac surgery). Note: The routine prophylactic use of lidocaine to prevent arrhythmia associated with fibrinolytic administration or to suppress isolated ventricular premature beats, couplets, runs of accelerated idioventricular rhythm, and nonsustained VT is not recommended. Ophthalmic: To provide local anesthesia to ocular surface during ophthalmologic procedures. Rectal: Temporary relief of pain and itching due to anorectal disorders. Topical: Local anesthetic for oral mucous membrane; use in laser/cosmetic surgeries; minor burns, cuts, and abrasions of the skin. Oral topical solution (viscous): Topical anesthesia of irritated oral mucous membranes and pharyngeal tissue. Patch (Lidoderm®): Relief of allodynia (painful hypersensitivity) and chronic pain in postherpetic neuralgia. Patch (LidoPatch™): Temporary relief of localized pain. ::: Unlabeled Uses: ACLS guidelines: Hemodynamically stable monomorphic ventricular tachycardia (VT) (preserved ventricular function); polymorphic VT (preserved ventricular function); drug-induced monomorphic VT; when amiodarone is not available, pulseless VT or ventricular fibrillation (VF) (unresponsive to defibrillation, CPR, and vasopressor administration). PALS guidelines: When amiodarone is not available, pulseless VT or VF (unresponsive to defibrillation, CPR, and epinephrine administration); consider in patients with cocaine overdose to prevent arrhythmias secondary to MI. I.V. infusion for chronic pain syndrome
benztropine
Trade name: Pharmacological Class: Anticholinergic for Treating Parkinson's Disease Mechanism of Action: Possesses both anticholinergic and antihistaminic effects. In vitro anticholinergic activity approximates that of atropine; in vivo it is only about half as active as atropine. Animal data suggest its antihistaminic activity and duration of action approach that of pyrilamine maleate. May also inhibit the reuptake and storage of dopamine, thereby prolonging the action of dopamine. Physiological Effects: Therapeutic Uses: Adjunctive treatment of Parkinson's disease; aid in the treatment of drug-induced extrapyramidal symptoms (except tardive dyskinesia)
flumazenil
Trade name: Pharmacological Class: Competitive GABA Receptor Antagonist Mechanism of Action: Competitively inhibits the activity at the benzodiazepine receptor site on the GABA/benzodiazepine receptor complex. Flumazenil does not antagonize the CNS effect of drugs affecting GABA-ergic neurons by means other than the benzodiazepine receptor (ethanol, barbiturates, general anesthetics) and does not reverse the effects of opioids Physiological Effects: Therapeutic Uses: Benzodiazepine antagonist; reverses sedative effects of benzodiazepines used in conscious sedation and general anesthesia; treatment of benzodiazepine overdose
procaine
Trade name: Pharmacological Class: Ester-type Local Anesthetic (Neuronal Membrane Permiability Modifier) Mechanism of Action: Ester local anesthetic blocks both the initiation and conduction of nerve impulses by decreasing the neuronal membrane's permeability to sodium ions, which results in inhibition of depolarization with resultant blockade of conduction; interferes with the uptake of norepinephrine by adrenergic nerve terminals producing vasoconstriction Physiological Effects: Therapeutic Uses: Topical anesthesia (and vasoconstriction) for mucous membranes
acetylcysteine
Trade name: Pharmacological Class: Glutathione Analog Mechanism of Action: Exerts mucolytic action through its free sulfhydryl group which opens up the disulfide bonds in the mucoproteins thus lowering mucous viscosity. Exerts mucolytic action through its free sulfhydryl group which opens up the disulfide bonds in the mucoproteins thus lowering mucous viscosity. The presumed mechanism in preventing contrast-induced nephropathy is its ability to scavenge oxygen-derived free radicals and improve endothelium-dependent vasodilation. Physiological Effects: Therapeutic Uses: Antidote for acute acetaminophen poisoning; repeated supratherapeutic ingestion (RSTI) of acetaminophen; adjunctive mucolytic therapy in patients with abnormal or viscid mucous secretions in acute and chronic bronchopulmonary diseases; pulmonary complications of surgery and cystic fibrosis; diagnostic bronchial studies ::: Unlabeled Uses: Prevention of contrast-induced renal dysfunction (oral, I.V.); distal intestinal obstruction syndrome (DIOS, previously referred to as meconium ileus equivalent)
sumatriptan
Trade name: IMITREX Pharmacological Class: Serotonin 5-HT1B,1D Receptor Agonist (Triptans) Mechanism of Action: Selective agonist for serotonin (5-HT1B and 5-HT1D receptors) in cranial arteries; causes vasoconstriction and reduces neurogenic inflammation associated with antidromic neuronal transmission correlating with relief of migraine. Physiological Effects: Therapeutic Uses: Intranasal, Oral, SubQ: Acute treatment of migraine with or without aura. SubQ: Acute treatment of cluster headache episodes.
buprenorphine
Trade name: Pharmacological Class: Mixed Mu Opioid Agonist-Antagonist Mechanism of Action: Buprenorphine exerts its analgesic effect via high affinity binding to μ opiate receptors in the CNS; displays partial mu agonist and weak kappa antagonist activity Physiological Effects: Therapeutic Uses: Injection: Management of moderate-to-severe pain. Sublingual tablet: Treatment of opioid dependence. Transdermal patch: Management of moderate-to-severe chronic pain in patients requiring an around-the-clock opioid analgesic for an extended period of time. ::: Unlabeled Uses: Injection: Management of opioid withdrawal in heroin-dependent hospitalized patients
selegiline
Trade name: Pharmacological Class: Monoamine Oxidase B Inhibitor Mechanism of Action: Potent, irreversible inhibitor of monoamine oxidase (MAO). Plasma concentrations achieved via administration of oral dosage forms in recommended doses confer selective inhibition of MAO type B, which plays a major role in the metabolism of dopamine; selegiline may also increase dopaminergic activity by interfering with dopamine reuptake at the synapse. When administered transdermally in recommended doses, selegiline achieves higher blood levels and effectively inhibits both MAO-A and MAO-B, which blocks catabolism of other centrally-active biogenic amine neurotransmitters. Physiological Effects: Therapeutic Uses: Adjunct in the management of parkinsonian patients in which levodopa/carbidopa therapy is deteriorating (oral products); treatment of major depressive disorder (transdermal product) ::: Unlabeled Uses: Early Parkinson's disease; attention-deficit/hyperactivity disorder (ADHD)
moclobemide
Trade name: Pharmacological Class: Reversible Inhibitor of Monoamine Oxidase A (RIMA) Mechanism of Action: Moclobemide is a benzamide derivative which acts as a short-acting reversible inhibitor of monoamine oxidase (MAO), which inhibits the metabolism (deamination) of serotonin, norepinephrine, and dopamine. It has a relative specificity for the A subtype of monoamine oxidase (MAO type A). Its action leads to increased concentrations of these neurotransmitters, which may account for the antidepressant activity of moclobemide. Physiological Effects: increased concentrations of serotonin, norepinephrine, and dopamine Therapeutic Uses: Symptomatic relief of depressive illness
donepezil
Trade name: ARICEPT Pharmacological Class: Centrally Acting Cholinesterase Inhibitor Mechanism of Action: Alzheimer's disease is characterized by cholinergic deficiency in the cortex and basal forebrain, which contributes to cognitive deficits. Donepezil reversibly and noncompetitively inhibits centrally-active acetylcholinesterase, the enzyme responsible for hydrolysis of acetylcholine. This appears to result in increased concentrations of acetylcholine available for synaptic transmission in the central nervous system. Physiological Effects: Therapeutic Uses: Treatment of mild, moderate, or severe dementia of the Alzheimer's type ::: Unlabeled Uses: Behavioral syndromes in dementia; mild-to-moderate dementia associated with Parkinson's disease; Lewy body dementia
aripiprazole
Trade name: Abilify Pharmacological Class: Atypical Antipsychotic Mechanism of Action: Aripiprazole is a quinolinone antipsychotic which exhibits high affinity for D2, D3, 5-HT1A, and 5-HT2A receptors; moderate affinity for D4, 5-HT2C, 5-HT7, alpha1 adrenergic, and H1 receptors. It also possesses moderate affinity for the serotonin reuptake transporter; has no affinity for muscarinic (cholinergic) receptors. Aripiprazole functions as a partial agonist at the D2 and 5-HT1A receptors, and as an antagonist at the 5-HT2A receptor. Physiological Effects: Therapeutic Uses: Oral: Acute and maintenance treatment of schizophrenia; acute (manic and mixed episodes) and maintenance treatment of bipolar I disorder as monotherapy or as an adjunct to lithium or valproic acid; adjunctive treatment of major depressive disorder; treatment of irritability associated with autistic disorder. Injection: Agitation associated with schizophrenia or bipolar I disorder (Abilify®); treatment of schizophrenia (Abilify Maintena™) ::: Unlabeled Uses: Depression with psychotic features; aggression (children); conduct disorder (children); Tourette syndrome (children); pervasive developmental disorder not otherwise specified (PDD-NOS) (children); Asperger's Disorder (children); psychosis/agitation related to Alzheimer's dementia
amphetamine/dextroamphetamine
Trade name: Adderall XR Pharmacological Class: Amphetamine Mechanism of Action: Amphetamines are noncatecholamine, sympathomimetic amines that promote release of catecholamines (primarily dopamine and norepinephrine) from their storage sites in the presynaptic nerve terminals. A less significant mechanism may include their ability to block the reuptake of catecholamines by competitive inhibition. Physiological Effects: Therapeutic Uses Attention-deficit/hyperactivity disorder (ADHD); narcolepsy
zolpidem
Trade name: Ambien Pharmacological Class: Non-BZD Hypnotic (Sleep Aid) Mechanism of Action: Zolpidem, an imidazopyridine hypnotic that is structurally dissimilar to benzodiazepines, enhances the activity of the inhibitory neurotransmitter, γ-aminobutyric acid (GABA), via selective agonism at the benzodiazepine-1 (BZ1) receptor; the result is increased chloride conductance, neuronal hyperpolarization, inhibition of the action potential, and a decrease in neuronal excitability leading to sedative and hypnotic effects. Because of its selectivity for the BZ1 receptor site over the BZ2 receptor site, zolpidem exhibits minimal anxiolytic, myorelaxant, and anticonvulsant properties (effects largely attributed to agonism at the BZ2 receptor site). Physiological Effects: Therapeutic Uses: Ambien®, Edluar™, Zolpimist®: Short-term treatment of insomnia (with difficulty of sleep onset) Ambien CR®: Treatment of insomnia (with difficulty of sleep onset and/or sleep maintenance) Intermezzo®: "As needed" treatment of middle-of-the-night insomnia with ≥4 hours of sleep time remaining.
disulfiram
Trade name: Antabuse Pharmacological Class: Aldehyde Dehydrogenase Inhibitor Mechanism of Action: Disulfiram is a thiuram derivative which interferes with aldehyde dehydrogenase. When taken concomitantly with alcohol, there is an increase in serum acetaldehyde levels. High acetaldehyde causes uncomfortable symptoms including flushing, nausea, thirst, palpitations, chest pain, vertigo, and hypotension. This reaction is the basis for disulfiram use in postwithdrawal long-term care of alcoholism. Physiological Effects: Therapeutic Uses: Management of chronic alcoholism
buspirone
Trade name: BuSpar Pharmacological Class: Serotonin 1A Partial Agonist Mechanism of Action: The mechanism of action of buspirone is unknown. Buspirone has a high affinity for serotonin 5-HT1A and 5-HT2 receptors, without affecting benzodiazepine-GABA receptors. Buspirone has moderate affinity for dopamine D2 receptors. Physiological Effects: Therapeutic Uses: Management of generalized anxiety disorder (GAD) ::: Unlabeled Uses: Management of aggression in mental retardation and secondary mental disorders; major depression; potential augmenting agent for antidepressants; premenstrual syndrome
clonidine
Trade name: Catapres Pharmacological Class: Centrally Acting Alpha2 Agonist (Indirect-Acting Alpha1/Beta1/Beta2 Inhibitor) Mechanism of Action: Stimulates alpha2-adrenoceptors in the brain stem, thus activating an inhibitory neuron, resulting in reduced sympathetic outflow from the CNS, producing a decrease in peripheral resistance, renal vascular resistance, heart rate, and blood pressure; epidural clonidine may produce pain relief at spinal presynaptic and postjunctional alpha2-adrenoceptors by preventing pain signal transmission; pain relief occurs only for the body regions innervated by the spinal segments where analgesic concentrations of clonidine exist. For the treatment of ADHD, the mechanism of action is unknown; it has been proposed that postsynaptic alpha2-agonist stimulation regulates subcortical activity in the prefrontal cortex, the area of the brain responsible for emotions, attentions, and behaviors and causes reduced hyperactivity, impulsiveness, and distractibility. Physiological Effects: Therapeutic Uses: Oral: Immediate release: Management of hypertension (monotherapy or as adjunctive therapy). Extended release (Kapvay™): Treatment of attention-deficit/hyperactivity disorder (ADHD) (monotherapy or as adjunctive therapy). Epidural (Duraclon®): For continuous epidural administration as adjunctive therapy with opioids for treatment of severe cancer pain in patients tolerant to or unresponsive to opioids alone; epidural clonidine is generally more effective for neuropathic pain and less effective (or possibly ineffective) for somatic or visceral pain. Transdermal patch: Management of hypertension (monotherapy or as adjunctive therapy). ::: Unlabeled Uses: Heroin or nicotine withdrawal; severe pain; dysmenorrhea; vasomotor symptoms associated with menopause; ethanol dependence; prophylaxis of migraines; glaucoma; diabetes-associated diarrhea; impulse control disorder, clozapine-induced sialorrhea; aid in the diagnosis of growth hormone deficiency; attention-deficit/hyperactivity disorder (ADHD) and associated insomnia in children; Tourette's syndrome in children; aggression associated with conduct disorder
varenicline
Trade name: Chantix Pharmacological Class: Partial Nicotine Agonist Mechanism of Action: Partial neuronal α4 β2 nicotinic receptor agonist; prevents nicotine stimulation of mesolimbic dopamine system associated with nicotine addiction. Also binds to 5-HT3 receptor (significance not determined) with moderate affinity. Varenicline stimulates dopamine activity but to a much smaller degree than nicotine does, resulting in decreased craving and withdrawal symptoms. Physiological Effects: Therapeutic Uses: Smoking cessation: Aid to smoking cessation treatment
valproic acid
Trade name: Depakene Pharmacological Class: Mood Stabilizing Anticonvulsant Mechanism of Action: Causes increased availability of gamma-aminobutyric acid (GABA), an inhibitory neurotransmitter, to brain neurons or may enhance the action of GABA or mimic its action at postsynaptic receptor sites Physiological Effects: Therapeutic Uses: Oral, I.V.: Monotherapy and adjunctive therapy in the treatment of patients with complex partial seizures; monotherapy and adjunctive therapy of simple and complex absence seizures; adjunctive therapy in patients with multiple seizure types that include absence seizures. Additional indications: Depakote®, Depakote® ER, Stavzor™: Mania associated with bipolar disorder; migraine prophylaxis. ::: Unlabeled Uses: Refractory status epilepticus, diabetic neuropathy
trazodone
Trade name: Desyrel, Oleptro Pharmacological Class: Serotonin 5HT2 Antagonist/Reuptake Inhibitor (SARI) Mechanism of Action: Inhibits reuptake of serotonin, causes adrenoreceptor subsensitivity, and induces significant changes in 5-HT presynaptic receptor adrenoreceptors. Trazodone also significantly blocks histamine (H1) and alpha1-adrenergic receptors. Physiological Effects: Inhibits reuptake of serotonin, significantly blocks histamine (H1) and alpha1-adrenergic receptors Therapeutic Uses: Treatment of major depressive disorder ::: Unlabeled Uses: Potential augmenting agent for antidepressants, hypnotic
venlafaxine
Trade name: Effexor XR Pharmacological Class: Serotonin/Norepinephrine Reuptake Inhibitor (SNRI) Mechanism of Action: Venlafaxine and its active metabolite, O-desmethylvenlafaxine (ODV), are potent inhibitors of neuronal serotonin and norepinephrine reuptake and weak inhibitors of dopamine reuptake. Venlafaxine and ODV have no significant activity for muscarinic cholinergic, H1-histaminergic, or alpha2-adrenergic receptors. Venlafaxine and ODV do not possess MAO-inhibitory activity. Physiological Effects: inhibitors of neuronal serotonin and norepinephrine reuptake and weak inhibitors of dopamine reuptake Therapeutic Uses: Treatment of major depressive disorder, generalized anxiety disorder (GAD), social anxiety disorder (social phobia), panic disorder ::: Unlabeled Uses: Obsessive-compulsive disorder (OCD); hot flashes; neuropathic pain (including diabetic neuropathy); attention-deficit/hyperactivity disorder (ADHD); post-traumatic stress disorder (PTSD); migraine prophylaxis
lithium
Trade name: Eskalith, Lithobid Pharmacological Class: Mood Stabilizing Monovalent Cation Mechanism of Action: Alters cation transport across cell membrane in nerve and muscle cells and influences reuptake of serotonin and/or norepinephrine; second messenger systems involving the phosphatidylinositol cycle are inhibited; postsynaptic D2 receptor supersensitivity is inhibited Physiological Effects: Therapeutic Uses: Management of bipolar disorders; treatment of mania in individuals with bipolar disorder (maintenance treatment prevents or diminishes intensity of subsequent episodes) ::: Unlabeled Uses: Potential augmenting agent for antidepressants; aggression, post-traumatic stress disorder, conduct disorder in children
butalbital/acetaminophen/caffeine
Trade name: Fioricet Pharmacological Class: Combination Barbiturate/Cox Inhibitor/CNS Stimulant (+/- Opioid Analgesic) Mechanism of Action: Butalbital is a short- to intermediate-acting barbiturate. Barbiturates depress the sensory cortex, decrease motor activity, alter cerebellar function, and produce drowsiness, sedation, hypnosis, and dose-dependent respiratory depression. Acetaminophen inhibits the synthesis of prostaglandins in the central nervous system and peripherally blocks pain impulse generation; produces antipyresis from inhibition of hypothalamic heat-regulating center. Caffeine increases levels of 3'5' cyclic AMP by inhibiting phosphodiesterase; CNS stimulant which increases medullary respiratory center sensitivity to carbon dioxide, stimulates central inspiratory drive, and improves skeletal muscle contraction (diaphragmatic contractility). Physiological Effects: Therapeutic Uses: Relief of the symptomatic complex of tension or muscle contraction headache
haloperidol
Trade name: Haldol Pharmacological Class: High Potency 1st Generation Antipsychotic Mechanism of Action: Haloperidol is a butyrophenone antipsychotic which blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain; depresses the release of hypothalamic and hypophyseal hormones; believed to depress the reticular activating system thus affecting basal metabolism, body temperature, wakefulness, vasomotor tone, and emesis Physiological Effects: Therapeutic Uses: Management of schizophrenia; control of tics and vocal utterances of Tourette's disorder in children and adults; severe behavioral problems in children ::: Unlabeled Uses: Treatment of nonschizophrenia psychosis; may be used for the emergency sedation of severely-agitated or delirious patients; adjunctive treatment of ethanol dependence; postoperative nausea and vomiting (alternative therapy); psychosis/agitation related to Alzheimer's dementia
guanfacine
Trade name: Intuniv Pharmacological Class: Alpha2-Adrenergic Agonist with Anti-ADHD Effects Mechanism of Action: Physiological Effects: Guanfacine is a selective alpha2A-adrenoreceptor agonist which reduces sympathetic nerve impulses, resulting in reduced sympathetic outflow and a subsequent decrease in vasomotor tone and heart rate. In addition, guanfacine preferentially binds postsynaptic alpha2A-adrenoreceptors in the prefrontal cortex and has been theorized to improve delay-related firing of prefrontal cortex neurons. As a result, underlying working memory and behavioral inhibition are affected; thereby improving symptoms associated with ADHD. Guanfacine is not a CNS stimulant. Therapeutic Uses: Tablet, immediate release: Management of hypertension. Tablet, extended release: Treatment of attention-deficit/hyperactivity disorder (ADHD) as monotherapy or adjunctive therapy to stimulants. ::: Unlabeled Uses: Tic disorder; Tourette's syndrome
escitalopram
Trade name: LEXAPRO Pharmacological Class: Selective Serotonin Reuptake Inhibitor (SSRI) Mechanism of Action: Escitalopram is the S-enantiomer of the racemic derivative citalopram, which selectively inhibits the reuptake of serotonin with little to no effect on norepinephrine or dopamine reuptake. It has no or very low affinity for 5-HT1-7, alpha- and beta-adrenergic, D1-5, H1-3, M1-5, and benzodiazepine receptors. Escitalopram does not bind to or has low affinity for Na+, K+, Cl-, and Ca++ ion channels. Physiological Effects: inhibits the reuptake of serotonin with little to no effect on norepinephrine or dopamine reuptake Therapeutic Uses: Treatment of major depressive disorder; generalized anxiety disorders (GAD) ::: Unlabeled Uses: Treatment of mild dementia-associated agitation in nonpsychotic patients; treatment of vasomotor symptoms associated with menopause
pregabalin
Trade name: Lyrica Pharmacological Class: CNS Voltage-Gated Calcium Channel Inhibitor Mechanism of Action: Binds to alpha2-delta subunit of voltage-gated calcium channels within the CNS, inhibiting excitatory neurotransmitter release. Although structurally related to GABA, it does not bind to GABA or benzodiazepine receptors. Exerts antinociceptive and anticonvulsant activity. Decreases symptoms of painful peripheral neuropathies and, as adjunctive therapy in partial seizures, decreases the frequency of seizures. Pregabalin may also affect descending noradrenergic and serotonergic pain transmission pathways from the brainstem to the spinal cord. Physiological Effects: Therapeutic Uses: Management of neuropathic pain associated with diabetic peripheral neuropathy or with spinal cord injury; management of postherpetic neuralgia; adjunctive therapy for partial-onset seizure disorder; management of fibromyalgia
dihydroergotamine
Trade name: MIGRANAL Pharmacological Class: Ergot Derivative Mechanism of Action: Ergot alkaloid alpha-adrenergic blocker directly stimulates vascular smooth muscle to vasoconstrict peripheral and cerebral vessels; also has effects on serotonin receptors Physiological Effects: Therapeutic Uses: Treatment of migraine headache with or without aura; injection also indicated for treatment of cluster headaches ::: Unlabeled Uses: Adjunct for DVT prophylaxis for hip surgery, for orthostatic hypotension, xerostomia secondary to antidepressant use, and pelvic congestion with pain
morphine sulfate
Trade name: MS Contin, KADIAN, Avinza Pharmacological Class: Strong Mu Opioid Agonist Mechanism of Action: Binds to opioid receptors in the CNS, causing inhibition of ascending pain pathways, altering the perception of and response to pain; produces generalized CNS depression Physiological Effects: Therapeutic Uses: Relief of moderate-to-severe acute and chronic pain; relief of pain of myocardial infarction; relief of dyspnea of acute left ventricular failure and pulmonary edema; preanesthetic medication. Infumorph: Used in continuous microinfusion devices for intrathecal or epidural administration in treatment of intractable chronic pain. Extended release products: Moderate-to-severe pain when continuous, around-the-clock opioid analgesia is needed for an extended period of time. Note: Opioid tolerance: Use of morphine sulfate extended release tablets/capsules ≥90 mg, and/or the oral solution 100 mg/5 mL (20 mg/mL) should be reserved for opioid-tolerant patients (ie, already taking at least 60 mg daily of oral morphine equivalent for at least 1 week).
acetaminophen/isometheptene/dichloralphenazone
Trade name: Midrin Pharmacological Class: Combination APAP/amine/ergot derivatives Mechanism of Action: Acetaminophen: Although not fully elucidated, believed to inhibit the synthesis of prostaglandins in the central nervous system and work peripherally to block pain impulse generation; produces antipyresis from inhibition of hypothalamic health-regulating center. Dichloralphenazone: Prodrug, converted to chloral hydrate (sedative) and antipyrine (analgesic/antipyretic) that reduces patient's emotional response to painful stimuli. Isometheptene: A sympathomimetic that reduces stimuli leading to vascular headaches via constriction of dilated cranial and cerebral arterioles. Physiological Effects: Therapeutic Uses: Relief of migraine and tension headache
memantine
Trade name: Namenda Pharmacological Class: N-Methyl-D-Aspartate Receptor Antagonist (NDMA Receptor Antagonist) Mechanism of Action: Glutamate, the primary excitatory amino acid in the CNS, may contribute to the pathogenesis of Alzheimer's disease (AD) by overstimulating various glutamate receptors leading to excitotoxicity and neuronal cell death. Memantine is an uncompetitive antagonist of the N-methyl-D-aspartate (NMDA) type of glutamate receptors, located ubiquitously throughout the brain. Under normal physiologic conditions, the (unstimulated) NMDA receptor ion channel is blocked by magnesium ions, which are displaced after agonist-induced depolarization. Pathologic or excessive receptor activation, as postulated to occur during AD, prevents magnesium from reentering and blocking the channel pore resulting in a chronically open state and excessive calcium influx. Memantine binds to the intra-pore magnesium site, but with longer dwell time, and thus functions as an effective receptor blocker only under conditions of excessive stimulation; memantine does not affect normal neurotransmission. Physiological Effects: Therapeutic Uses: Treatment of moderate-to-severe dementia of the Alzheimer's type ::: Unlabeled Uses: Treatment of mild-to-moderate vascular dementia
phenelzine
Trade name: Nardil Pharmacological Class: Classical Monoamine Oxidase Inhibitor Mechanism of Action: Thought to act by increasing endogenous concentrations of norepinephrine, dopamine, and serotonin through inhibition of the enzyme (monoamine oxidase) responsible for the breakdown of these neurotransmitters Physiological Effects: increased endogenous concentrations of norepinephrine, dopamine, and serotonin Therapeutic Uses: Symptomatic treatment of atypical, nonendogenous, or neurotic depression
gabapentin
Trade name: Neurontin, Gabarone Pharmacological Class: Analeptics Without Mood-Stabilizing Effects Mechanism of Action: Gabapentin is structurally related to GABA. However, it does not bind to GABAA or GABAB receptors, and it does not appear to influence synthesis or uptake of GABA. High affinity gabapentin binding sites have been located throughout the brain; these sites correspond to the presence of voltage-gated calcium channels specifically possessing the alpha-2-delta-1 subunit. This channel appears to be located presynaptically, and may modulate the release of excitatory neurotransmitters which participate in epileptogenesis and nociception. Physiological Effects: Therapeutic Uses: Adjunct for treatment of partial seizures with and without secondary generalized seizures in patients >12 years of age with epilepsy; adjunct for treatment of partial seizures in pediatric patients 3-12 years of age; management of postherpetic neuralgia (PHN) in adults ::: Unlabeled Uses: Neuropathic pain, diabetic peripheral neuropathy, fibromyalgia, postoperative pain (adjunct), restless legs syndrome (RLS), vasomotor symptoms
oxycodone
Trade name: OxyContin, Roxicodone, Endocet Pharmacological Class: Moderate-to-Weak Mu Opioid Agonist Mechanism of Action: Binds to opiate receptors in the CNS, causing inhibition of ascending pain pathways, altering the perception of and response to pain; produces generalized CNS depression. Physiological Effects: Therapeutic Uses: Management of moderate-to-severe pain, normally used in combination with nonopioid analgesics. OxyContin® is indicated for around-the-clock management of moderate-to-severe pain when a continuous analgesic is needed for an extended period of time.
nortriptyline
Trade name: Pamelor Pharmacological Class: Secondary Amine Tricyclic Antidepressant Mechanism of Action: Traditionally believed to increase the synaptic concentration of serotonin and/or norepinephrine in the central nervous system by inhibition of their reuptake by the presynaptic neuronal membrane. However, additional receptor effects have been found including desensitization of adenyl cyclase, down regulation of beta-adrenergic receptors, and down regulation of serotonin receptors. Physiological Effects: increase the synaptic concentration of serotonin and/or norepinephrine Therapeutic Uses: Treatment of symptoms of depression ::: Unlabeled Uses: Chronic pain (including neuropathic pain), myofascial pain, burning mouth sydrome, anxiety disorders, attention-deficit/hyperactivity disorder (ADHD); enuresis; adjunctive therapy for smoking cessation
modafinil
Trade name: Provigil Pharmacological Class: Modafinil Mechanism of Action: The exact mechanism of action is unclear, it does not appear to alter the release of dopamine or norepinephrine, it may exert its stimulant effects by decreasing GABA-mediated neurotransmission, although this theory has not yet been fully evaluated; several studies also suggest that an intact central alpha-adrenergic system is required for modafinil's activity; the drug increases high-frequency alpha waves while decreasing both delta and theta wave activity, and these effects are consistent with generalized increases in mental alertness Physiological Effects: Therapeutic Uses: Improve wakefulness in patients with excessive daytime sleepiness associated with narcolepsy and shift work sleep disorder (SWSD); adjunctive therapy for obstructive sleep apnea/hypopnea syndrome (OSAHS) ::: Unlabeled Uses: Attention-deficit/hyperactivity disorder (ADHD); treatment of fatigue in MS and other disorders
mirtazapine
Trade name: Remeron Pharmacological Class: Noradrenergic and Specific Serotonergic Antidepressant (NaSSA) Mechanism of Action: Mirtazapine is a tetracyclic antidepressant that works by its central presynaptic alpha2-adrenergic antagonist effects, which results in increased release of norepinephrine and serotonin. It is also a potent antagonist of 5-HT2 and 5-HT3 serotonin receptors and H1 histamine receptors and a moderate peripheral alpha1-adrenergic and muscarinic antagonist; it does not inhibit the reuptake of norepinephrine or serotonin. Physiological Effects: increased release of norepinephrine and serotonin Therapeutic Uses: Treatment of depression ::: Unlabeled Uses: Alzheimer's dementia-related depression; post-traumatic stress disorder (PTSD)
ramelteon
Trade name: Rozerem Pharmacological Class: Melatonin Receptor Agonist Mechanism of Action: Potent, selective agonist of melatonin receptors MT1 and MT2 (with little affinity for MT3) within the suprachiasmic nucleus of the hypothalamus, an area responsible for determination of circadian rhythms and synchronization of the sleep-wake cycle. Agonism of MT1 is thought to preferentially induce sleepiness, while MT2 receptor activation preferentially influences regulation of circadian rhythms. Ramelteon is eightfold more selective for MT1 than MT2 and exhibits nearly sixfold higher affinity for MT1 than melatonin, presumably allowing for enhanced effects on sleep induction. Physiological Effects: induce sleepiness Therapeutic Uses: Treatment of insomnia characterized by difficulty with sleep onset
naloxone
Trade name: Suboxone Pharmacological Class: Competitive Mu Opioid Receptor Antagonist Mechanism of Action: Pure opioid antagonist that competes and displaces narcotics at opioid receptor sites Physiological Effects: Therapeutic Uses: Complete or partial reversal of opioid drug effects, including respiratory depression; management of known or suspected opioid overdose; diagnosis of suspected opioid dependence or acute opioid overdose ::: Unlabeled Uses: Opioid-induced pruritus
amantadine
Trade name: Symmetrel Pharmacological Class: Dopamine Agonist Mechanism of Action: As an antiviral, blocks the uncoating of influenza A virus preventing penetration of virus into host; antiparkinsonian activity may be due to its blocking the reuptake of dopamine into presynaptic neurons or by increasing dopamine release from presynaptic fibers Physiological Effects: Therapeutic Uses: Prophylaxis and treatment of influenza A viral infection (per manufacturer labeling; also refer to current ACIP guidelines for recommendations during current flu season); treatment of parkinsonism; treatment of drug-induced extrapyramidal symptoms
chlorpromazine
Trade name: Thorazine Pharmacological Class: Low Potency 1st Generation Antipsychotic Mechanism of Action: Chlorpromazine is an aliphatic phenothiazine antipsychotic which blocks postsynaptic mesolimbic dopaminergic receptors in the brain; exhibits a strong alpha-adrenergic blocking effect and depresses the release of hypothalamic and hypophyseal hormones; believed to depress the reticular activating system, thus affecting basal metabolism, body temperature, wakefulness, vasomotor tone, and emesis Physiological Effects: Therapeutic Uses: Management of psychotic disorders (control of mania, treatment of schizophrenia); control of nausea and vomiting; relief of restlessness and apprehension before surgery; acute intermittent porphyria; adjunct in the treatment of tetanus; intractable hiccups; combativeness and/or explosive hyperexcitable behavior in children 1-12 years of age and in short-term treatment of hyperactive children ::: Unlabeled Uses: Behavioral symptoms associated with dementia (elderly); psychosis/agitation related to Alzheimer's dementia
imipramine
Trade name: Tofranil Pharmacological Class: Tertiary Amine Tricyclic Antidepressant Mechanism of Action: Traditionally believed to increase the synaptic concentration of serotonin and/or norepinephrine in the central nervous system by inhibition of their reuptake by the presynaptic neuronal membrane. However, additional receptor effects have been found including desensitization of adenyl cyclase, down regulation of beta-adrenergic receptors, and down regulation of serotonin receptors. Physiological Effects: increase the synaptic concentration of serotonin and/or norepinephrine Therapeutic Uses: Treatment of depression; treatment of nocturnal enuresis in children ::: Unlabeled Uses: Analgesic for certain chronic and neuropathic pain (including diabetic neuropathy); panic disorder; attention-deficit/hyperactivity disorder (ADHD); post-traumatic stress disorder (PTSD)
acetaminophen
Trade name: Tylenol Pharmacological Class: Centrally Acting Cyclooxygenase Inhibitor Mechanism of Action: Although not fully elucidated, believed to inhibit the synthesis of prostaglandins in the central nervous system and work peripherally to block pain impulse generation; produces antipyresis from inhibition of hypothalamic heat-regulating center Physiological Effects: Therapeutic Uses: Treatment of mild-to-moderate pain and fever (analgesic/antipyretic). I.V.: Additional indication: Management of moderate-to-severe pain when combined with opioid analgesia.
tramadol
Trade name: Ultram ER Pharmacological Class: Mixed Weak Mu Opioid Agonist/Norepinepherine Transporter Inhibitor Mechanism of Action: Tramadol and its active metabolite (M1) binds to μ-opiate receptors in the CNS causing inhibition of ascending pain pathways, altering the perception of and response to pain; also inhibits the reuptake of norepinephrine and serotonin, which also modifies the ascending pain pathway. Physiological Effects: Therapeutic Uses: Relief of moderate to moderately-severe pain. Extended release formulations are indicated for patients requiring around-the-clock management of moderate to moderately-severe pain for an extended period of time.
hydrocodone/acetaminophen
Trade name: Vicodin, Lortab Pharmacological Class: Combination Opioid/Nonopioid Analgesics Mechanism of Action: Hydrocodone, as with other narcotic (opiate) analgesics, blocks pain perception in the cerebral cortex by binding to specific receptor molecules (opiate receptors) within the neuronal membranes of synapses. This binding results in a decreased synaptic chemical transmission throughout the CNS thus inhibiting the flow of pain sensations into the higher centers. Mu and kappa are the two subtypes of the opiate receptor which hydrocodone binds to cause analgesia. Acetaminophen inhibits the synthesis of prostaglandins in the CNS and peripherally blocks pain impulse generation; produces antipyresis from inhibition of hypothalamic heat-regulating center. Physiological Effects: Therapeutic Uses: Relief of moderate-to-severe pain
bupropion
Trade name: Wellbutrin, Budeprion, Zyban Pharmacological Class: Norepinephrine/Dopamine Reuptake Inhibitor (NDRI ) Mechanism of Action: Aminoketone antidepressant structurally different from all other marketed antidepressants; like other antidepressants the mechanism of bupropion's activity is not fully understood. Bupropion is a relatively weak inhibitor of the neuronal uptake of norepinephrine and dopamine, and does not inhibit monoamine oxidase or the reuptake of serotonin. Metabolite inhibits the reuptake of norepinephrine. The primary mechanism of action is thought to be dopaminergic and/or noradrenergic. Physiological Effects: weak inhibitor of the neuronal uptake of norepinephrine and dopamine, and does not inhibit monoamine oxidase or the reuptake of serotonin. Metabolite inhibits the reuptake of norepinephrine Therapeutic Uses: Treatment of major depressive disorder, including seasonal affective disorder (SAD); adjunct in smoking cessation (Buproban®, Zyban®) ::: Unlabeled Uses: Attention-deficit/hyperactivity disorder (ADHD); depression associated with bipolar disorder
alprazolam
Trade name: Xanax Pharmacological Class: Bezodiazepines Mechanism of Action: Binds to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron at several sites within the central nervous system, including the limbic system, reticular formation. Enhancement of the inhibitory effect of GABA on neuronal excitability results by increased neuronal membrane permeability to chloride ions. This shift in chloride ions results in hyperpolarization (a less excitable state) and stabilization. Physiological Effects: Enhancement of the inhibitory effect of GABA Therapeutic Uses: Treatment of anxiety disorder (GAD); short-term relief of symptoms of anxiety; panic disorder, with or without agoraphobia; anxiety associated with depression
