Q3Grp2 Flashcards
Buspirone
Brand: Buspar
Class: Antianxiety
MOA: first of a class of selective serotonin-5-HT1A receptor partial agonists. It also has some effect on dopamine-D2 auto-receptors and, like antidepressants, can downregulate β-adrenergic receptors. Unlike benzodiazepines, it lacks amnestic, anticonvulsant, muscle relaxant, and hypnotic effects. Its exact anxiolytic mechanism of action is complex and not clearly defined.
Indication: Anxiety
Contraindication: Hypersens
Black Box: N/A
Preg: Low Risk
Counseling Pts: Patient should avoid activities requiring mental alertness or coordination until drug effects are realized. Advise patient that symptomatic improvement may not be seen for a few weeks. Advise patient against sudden discontinuation of drug. Patient may take with or without food, but should always take drug consistently. Patient should not drink alcohol or large amounts of grapefruit juice while taking this drug. Avoid concomitant use with MAOI.
Levetiracetam
Brand: Keppra
Class: Anticonvulsant
MOA: A pyrrolidine derivative that is structurally unrelated to other AEDs. Its mechanism of action is unclear and does not relate to any known mechanisms of neuronal excitation or inhibition. The action of levetiracetam in animal models of seizures and epilepsy is unique from other AEDs.
Indication: Seizure
Contraindication: Hypersens
Black Box: N/A
Preg: Probably Compatible
Counseling Pts: Safety and efficacy of extended-release tablet not established in children <16 y of age. Patients weighing <20 kg should receive the oral solution. Data suggest an increased risk of suicidal behavior, or ideation may exist in patients receiving therapy with AEDs. Pregnancy: up to a 50% dose increase during 3rd trimester with subsequent dose reduction after delivery may be necessary. Do not stop abruptly; increased risk of seizures. Dispense with medication safety guideline. Injectable formulation also available
Mirtazapine
Brand: Remeron
Class: Antidepressant, α2-Antagonist
MOA: an antidepressant that antagonizes presynaptic α2-adrenergic auto- and heteroreceptors that are responsible for controlling the release of norepinephrine and serotonin (5-HT). It is also a potent antagonist of postsynaptic 5-HT2 and 5-HT3 receptors. The net outcome of these effects is increased noradrenergic activity and enhanced 5-HT activity, especially at 5-HT1A receptors. This unique mechanism of action preserves antidepressant efficacy but minimizes many of the adverse effects common to heterocyclic antidepressants and SSRIs.
Indication: Depression
Contraindication: Hypersensitivity to mirtazapine; concurrent use or use within 14 d of MAOI, linezolid, IV methylene blue use.
Black Box: Suicidality. NOT FOR KIDS
Preg: Moderate Risk
Counseling Pts: Orally disintegrating tablet blister pack should be opened with dry hands and placed on tongue; no water is needed; tablet should be used immediately after removal from package; once removed, it cannot be stored. Avoid activities requiring mental alertness until drug effects are realized. Report worsening depression, suicidal ideation, or unusual changes in behavior. Do not drink alcohol while taking this drug. Take in the evening prior to sleep.
Aripiprazole
Brand: Abilify
Class: Antipsychotic
MOA: An atypical antipsychotic agent (quinolinone derivative). It exhibits partial agonist activity at dopamine D2 and D3 receptors and serotonin 5-HT1A receptors and antagonist activity at 5-HT2A receptors.
Indication: Bipolar, Schizophrenia, Depression (adjunctive), Tourette’s, Autism+Irritability
Contraindication: Hypersens
Black Box: Dementia, Suicidality
Preg: Low Risk
Counseling Pts: Avoid activities requiring mental alertness or coordination until drug effects are realized. Drug may impair heat regulation. Drug may also lower seizure threshold. Patients with history of seizures or conditions that lower seizure threshold should report increased seizure activity. Report worsening depression, suicidal ideation, or unusual changes in behavior, especially at initiation of therapy or with dose changes. Children, adolescents, and young adults are at higher risk for these effects during the first few months of therapy. Report signs/symptoms of hyperglycemia, extrapyramidal effects, and neuroleptic malignant syndrome. Avoid sudden discontinuation. Avoid alcohol.
Sumatriptan
Brand: Imitrex
Class: Antimigraine Serotonin Receptor Agonist
MOA: binds with high affinity to serotonin (5-HT) subtypes 1B, 1D, and 1F receptors. It has no significant affinity or pharmacologic activity at adrenergic α1, α2, or β; dopaminergic D1 or D2; muscarinic; or opioid receptors. Serotonin receptor agonists are believed to be effective in migraine either through vasoconstriction (via activation of 5-HT1 receptors located on intracranial blood vessels) or through activation of 5-HT1 receptors on sensory nerve endings in the trigeminal system resulting in the inhibition of proinflammatory neuropeptide release.
Indication: Migraine, Cluster headaches
Contraindication: Hypersensitivity to sumatriptan, cerebrovascular syndromes, hemiplegic or basilar migraine, ischemic bowel disease, ischemic heart disease, peripheral vascular disease, severe hepatic impairment, uncontrolled HTN, MAOIs, ergot alkaloids
Black Box: N/A
Preg: Moderate Risk
Counseling Pts: Avoid activities requiring mental alertness or coordination until drug effects are realized, as this drug may cause dizziness or somnolence.
Diazepam
Brand: Valium
Class: Benzodiazepine C4
MOA: Enhanced postsynaptic effect of the inhibitory neurotransmitter, 𝛾-aminobutyric acid (GABA)
Indication: Alcohol Withdrawal Syndrome, Anxiety, Seizure
Contraindication: Hypersensitivity to benzodiazepines, narrow-angle glaucoma, severe liver disease, myasthenia gravis, sleep apnea, respiratory insufficiency, children <6 mo
Black Box: Concurrent use with opioids
Preg: Risk 1st/3rd Trimester
Counseling Pts: May cause drowsiness; avoid driving or other tasks requiring motor coordination. Avoid alcohol.
Ropinirole
Brand: Requip
Class: Dopamine Agonist
MOA: A nonergoline dopamine agonist that has a higher specificity to D3 than to D2 and D4 subtypes of dopamine receptors. The drug has a moderate affinity for opioid receptors and has insignificant effects on D1, 5-hydroxytryptamine 1 (5-HT1), 5-HT2, benzodiazepine, GABA, muscarinic, α1-, α2-, and β-adrenoreceptors. It is suggested that ropinirole stimulates the postsynaptic D2-type receptor found in the brain’s caudate putamen in Parkinson disease.
Indication: Parkinson’s and Restless Legs Syndrome.
Contraindication: Hypersens
Black Box: N/A
Preg: Risk
Counseling Pts: Take with food to reduce nausea. Avoid driving and other activities requiring mental alertness or coordination until drug effects are realized. Rise slowly from sitting/lying-down position. Report new onset or exacerbation of dyskinesia, changes in BP, fainting, or unusual urges. Avoid sudden discontinuation of drug; it increases risk of neuroleptic malignancy syndrome. Do not drink alcohol or take other CNS depressants while using this drug.
Guanfacine
Brand: Intuniv
Class: α2-Adrenergic Agonist
MOA: Guanfacine stimulates postsynaptic α2-adrenergic receptors in the CNS by activating inhibitory neurons to decrease sympathetic outflow.
Indication: ADHD in adolescents, HTN
Contraindication: Hypersens
Black Box: N/A
Preg: Low Risk
Counseling Pts: Avoid alcohol, CNS depressants. Caution with driving and other tasks requiring alertness. Swallow extended-release tablet whole, may be taken with or without food. Report signs/symptoms of hypotension, exacerbation of angina peripheral edema, fatigue, hypotension, or hepatic dysfunction with initial dosing and dose changes. Avoid abrupt discontinuation to avoid rebound HTN.
Donepezil
Brand: Aricept
Class: Central Cholinesterase Inhibitor
MOA: Enhances the action of acetylcholine by reversibly inhibiting acetylcholinesterase (AChE), the enzyme responsible for its hydrolysis. It has a high degree of selectivity for AChE in the CNS, which might explain the relative lack of peripheral side effects.
Indication: Alzheimer’s
Contraindication: Hypersensitivity to donepezil or piperidine derivatives
Black Box: N/A
Preg: Low Risk
Counseling Pts: Take at bedtime, with or without food. Allow disintegrating tablet to dissolve on tongue and follow with a glass of water. Adverse effects may be more frequent at dose escalation and tend to resolve with continued use. Report signs/symptoms of GI bleeding.
Nortriptyline
Brand: Pamelor
Class: Tricyclic Antidepressant
MOA: The demethylated metabolite of amitriptyline, a heterocyclic antidepressant that blocks presynaptic reuptake of norepinephrine with subsequent downregulation of adrenergic receptors. Heterocyclic antidepressants have less effect on serotonergic activity than on other neurotransmitters.
Indication: Depression
Contraindication: Hypersensitivity to nortriptyline or other TCAs; MAOI concurrent use or use within 14 d; use during acute recovery period after MI, patient using linezolid or IV methylene blue
Black Box: Suicidality
Preg: Low Risk
Counseling Pts: Avoid activities requiring mental alertness or coordination until drug effects are realized, as drug may cause somnolence and dizziness. Report worsening depression, suicidal ideation, unusual changes in behavior, or unusual bleeding. Avoid abrupt discontinuation; may precipitate withdrawal symptoms. Do not drink alcohol while taking this drug.
Divalproex Sodium
Brand: Depakote
Class: Anticonvulsant
MOA: Composed of sodium valproate and valproic acid. Valproic acid is a carboxylic acid compound whose anticonvulsant activity might be mediated by an inhibitory neurotransmitter, GABA. Valproic acid might increase GABA levels by inhibiting GABA metabolism or enhancing postsynaptic GABA activity. Valproic acid also limits repetitive neuronal firing through voltage- and usage-dependent sodium channels.
Indication: Seizure, Bipolar, Migraine Prophylaxis
Contraindication: Hypersensitivity to divalproex, hepatic disease, urea cycle disorders
Black Box: Hepatotoxicity, patients with mitochondrial disease, teratogenicity, pancreatitis
Preg: Risk
Counseling Pts: Avoid activities requiring mental alertness until drug effects are realized; drug may cause somnolence or dizziness. Seek medical attention for signs and symptoms of liver dysfunction (eg, dark-colored urine, light-colored stools, yellowing of skin or eyes, etc), especially during first 6 mo of therapy. Take with food to avoid GI irritation. Do not discontinue drug abruptly, as this may precipitate seizures. Avoid alcohol. Sprinkle capsules can be swallowed whole or opened and sprinkled onto soft food; do not chew.
Tamsulosin
Brand: Flomax
Class: α1-Adrenergic Blocker
MOA: closely related to quinazoline derivatives that selectively block postsynaptic α1-adrenergic receptors. Total peripheral resistance is reduced through arterial and venous dilations. Reflex tachycardia that occurs with other vasodilators is infrequent because there is no presynaptic α2-receptor blockade. The drugs also decrease total cholesterol, increase HDL-cholesterol, and may improve glucose tolerance and reduce left ventricular mass during long-term therapy. They increase urine flow in BPH by relaxing smooth muscle tone in the bladder neck and prostate.
Indication: Prostatic Hyperplasia (Enlarged Prostate)
Contraindication: Hypersens
Black Box: N/A
Preg: Low Risk
Counseling Pts: Administer 30 min after same meal daily as fasting increases bioavailability by 30%. Avoid activities requiring coordination until drug effects are realized, as drug may cause vertigo or dizziness. Rise slowly from a sitting/lying position, as this drug may cause orthostatic hypotension. Syncope or loss of consciousness is possible with 1st dose or dose increases, especially if in an upright position.
Allopurinol
Brand: Zyloprim
Class: Xanthine Oxidase Inhibitor; Antigout
MOA: Decreases the production of uric acid by inhibiting the action of xanthine oxidase, the enzyme that converts hypoxanthine to xanthine and xanthine to uric acid.
Indication: Gout, Kidney Stones, Hyperuricemia
Contraindication: Hypersens, concurrent use of didanosine
Black Box: N/A
Preg: No Data
Counseling Pts: Take after meals to lessen gastric irritation. Maintain adequate hydration during therapy to prevent kidney stones. Patient should avoid alcohol and caffeine while taking allopurinol. Seek medical attention if signs and symptoms of myelosuppression, agranulocytosis (severe neutropenia), or Stevens-Johnson syndrome (flulike symptoms, spreading red rash, or skin/mucous membrane blistering) occur.
Pregabalin
Brand: Lyrica
Class: Analgesic, Anticonvulsant. C-V
MOA: A GABA analogue that strongly binds to the α2-delta site (a subunit of voltage-gated calcium channels) in CNS tissues. Binding to the α2-delta subunit may be involved in pregabalin’s effects on neuropathic pain and seizure control. Pregabalin reduces the calcium-dependent release of several neurotransmitters; however, the exact mechanism of action is unknown.
Indication: Neuropathic pain, Fibromyalgia, Postherpetic neuralgia
Contraindication: Hypersens
Black Box: N/A
Preg: Moderate Risk
Counseling Pts: Solution must be used within 45 d of first opening the bottle. Avoid activities requiring mental alertness or coordination until drug effects are realized. Avoid sudden discontinuation of drug due to risk of withdrawal, including increased seizure frequency. Avoid concurrent use of CNS depressants, such as alcohol.
Diltiazem
Brand: Cardizem
Class: Ca Channel Blocker
MOA: A calcium-channel-blocking drug that decreases HR, prolongs AV nodal conduction, and decreases arteriolar and coronary vascular tone. It also has negative inotropic properties.
Indication: Angina, HTN, Atrial Fibrilation
Contraindication: Hypersensitivity to diltiazem, hypotension, 2nd- or 3rd-degree AV block, sick sinus syndrome
Black Box: N/A
Preg: Low Risk
Counseling Pts: Report symptomatic hypotension, bradyarrhythmia, peripheral edema, or syncope. This drug is available in multiple brand names with varying properties by brand. Instruct patient to follow administration instructions specific to the prescribed brand with regards to meals and timing. Do not drink alcohol while taking this drug. Some products may be opened and sprinkled on a spoonful of applesauce (applesauce should not be hot, and should be swallowed without chewing, followed by a glass of water). Administer at same time of day, either morning or evening.
