Pharm II - Test 2 Flashcards
Which antidepressant class has the most significant side effects profile?
Monoamine oxidase inhibitors (MAOI)
Which antidepressant class requires dietary recommendations (restriction of tyramine-containing foods)
Monoamine oxidase inhibitors (MAOI)
What is the risk of combining MAOIs with foods high in tyramine?
MAO usually breaks down tyramine -> Inc. absorption of intact tyramine -> toxic elevation of catecholamines -> severe HA, N, HTN (potentially hypertensive emergencies)
Class: Amitriptyline (Elavil)
Tricyclic antidepressant
Indication: Amitriptyline (Elavil)
Major depression, bipolar d/o, migraine/tension HA (prophylaxis), chronic pain
MOA: Amitriptyline (Elavil)
CNS modulation of both serotonin and norepinephrine
Side effects: Amitriptyline (Elavil)
Anticholinergic effects (dry mouth, constipation, urinary hesistancy, blurred vision)
Which antidepressant does not have the side effect of weight gain?
Wellbutrin
Class: Trazodone (Desyrel)
Tetracyclic antidepressant
Indication: Trazodone (Desyrel)
MDD, anxiety, panic disorder, insomnia
MOA: Trazodone (Desyrel)
Serotonin reuptake inhibitor and partial antagonist (SARI)
Class: Fluoxetine (Prozac)
Selective serotonin reuptake inhibitor (SSRI)
Indication: Fluoxetine (Prozac)
MDD, OCD, bulimia, panic disorder
MOA: Fluoxetine (Prozac)
Dec serotonin reuptake at presynaptic cleft -> inc serotonin for neurotransmission
Side effects: Fluoxetine (Prozac)
Serotonin syndrome (fever, agitation, D, hypertension), sexual dysfxn (dec libido, impotency, anorgasmia)
What drugs can interfere and reduce the efficiency of SSRIs?
Aspirin, Ibuprofen, Naproxen
Class: Duloxetine (Cymbalta)
Serotonin and norepinephrine reuptake inhibitor (SNRI)
Indication: Duloxetine (Cymbalta)
MDD, general anxiety, PAINFUL PERIPHERAL NEUROPATHY, FIBROMYALGIA
Class: Bupropion (Wellbutrin)
Norepinephrine and dopamine reuptake inhibitors (NDRI) and nicotine receptor antagonist
Indication: Bupropion (Wellbutrin)
MDD, bipolar do, ADD, smoking cessation (Zyban)
MOA: Bupropion (Wellbutrin)
Blockade of NE and DOPA reuptake
Addition of what nutrient may improve SSRI response?
Folic acid
What is the brand name of activated folic acid?
Deplin
Ultra-short acting barbiturate
Thiopental (Pentothal)
Short-acting barbiturate
Pentobarbital (Nembutal)
Intermediate-acting barbiturate
Butalbital (Fiorinal)
Long-acting barbiturate
Phenobarbital (Luminal)
What is the most widely used anticonvulsant worldwide?
Phenobarbital (Luminal)
What are the most widely used group of anxiolytic drugs?
Benzodiazepines
Indication: Midazolam (Versed)
Sedation/anxiety prior to upper/lower GI endoscopy
Acute mgmt of aggressive, violent, or delirious patients
Midazolam (Versed) is not indicated for ___.
long-term mgmt of seizure disorders
Class: Diazepam (Valium)
Benzodiazepine anticonvulsant
Indication: Diazepam (Valium)
Anxiolytic, sedative, muscle relaxant, STATUS EPILEPTICUS
MOA: Diazepam (Valium)
Binds to benzodiazepine receptors in CNS to enhance GABA activity -> inc Cl- influx -> inhibition of CNS synaptic transmission
MOA: Benzodiazepine-like sedatives
Increase GABA receptor affinity for GABA by binding to site different than benzo or barbiturate site
Class: Zolpidem (Ambien)
Short-acting, non-benzodiazepine hypnotic
Class: Eszopiclone (Lunesta)
Benzodiazepine-like hypnotic
Indications: Zolpidem (Ambien)
Trouble falling asleep, but not necessarily maintaining sleep
Indication: Eszopiclone (Lunesta)
Insomnia
MOA: Eszopiclone (Lunesta)
Potentiation of GABA effect on Cl- ion channels
Class: Ramelteon (Rozerem)
Melatonin receptor agonist
Class: Fumazenil (Romazicon)
Benzodiazepine receptor antagonist
Indication: Fumazenil (Romazicon)
Reverse effects of benzos
The chief antipsychotic effects of neuroleptics appear related to blockade of ___ in the ___
dopamine D2 receptors, mesolimbic pathway
Neuroleptic malignant syndrome
Rare side effect of neuroleptic use characterized by catatonia, fluctuating BP, dysarthria, fever
Tx: Neuroleptic malignant syndrome
Dopamine agonist (Bromocriptine)
Class: Chlorpromazine (Thorazine)
Typical neuroleptic
MOA: Chlorpromazine (Thorazine)
D2 dopaminergic receptor blocker
Alpha-adrenergic blocker
H1-histamine blocker
Side effect: Chlorpromazine (Thorazine)
INC RELEASE OF PRL
Neuroleptic side effects (Sedation, dizziness, HA, D, Extrapyramidal effects)
Class: Prochlorperazine (Compazine)
Typical neuroleptic
Indication: Prochlorperazine (Compazine)
Better anti-emetic than other neuroleptics
MOA: Prochlorperazine (Compazine)
H1-histaine receptor antagonist
Alpha-adrenergic receptor antagonist
D2 dopaminergic receptor antagonist
Class: Haloperidol (Haldol)
Typical neuroleptic
Indication: Haloperidol (Haldol)
Psychosis, Tourette’s syndrome, Huntington’s disease, ACUTE AGITATED BEHAVIOR
MOA: Haloperidol (Haldol)
D2 dopamine receptor blocker
Side effects: Haloperidol (Haldol)
neuroleptic malignant syndrome
Class: Clozapine (Clozaril)
Atypical neuroleptic
Indication: Clozapine (Clozaril)
Schizophrenia, esp. when other anti-psychotics have failed (3rd line)
MOA: Clozapine (Clozaril)
Multiple receptor site blockage, greatest at D2 and 5-HT2 serotonin sites
Class: Respiradone (Risperdal)
Atypical neuroleptic
Side effects: Respiradone (Risperdal)
WEIGHT GAIN, HYPERGLYCEMIA, DIABETES, extrapyramidal effects, tardive dyskinesia, sedation, INC RISK FOR STROKE IN ELDERLY
Class: Olanzapine (Zyprexa)
Atypical neuroleptic
MOA: Olanzapine (Zyprexa)
Multiple site blocker (esp. D2 and 5-HT2)
Side effects: Olanzapine (Zyprexa)
WEIGHT GAIN, HYPERGLYCEMIA, DIABETES, INC RISK FOR STROKE IN ELDERLY
Side effects: Lithium carbonate (Eskalith)
NEPHROGENIC DIABETES INSIPIDUS
IMPAIRED CONCENTRATION CAPACITY DT REDUCED RENAL RESPONSE TO ADH
HYPOTHYROIDISM
Class: Phenobarbital (Phenobarb)
Barbiturate anticonvulsant
MOA: Phenobarbital (Phenobarb)
Enhanced GABA activity
Which drug mb the initial drug of choice in children with seizures?
Phenobarbital (Phenobarb)
Side effects: Phenobarbital (Phenobarb)
lower IQ scores in children
Class: Primidone (Mysoline)
Barbiturate anticonvulsant
MOA: Primidone (Mysoline)
Pro-drug of phenobarbital
Contraindications: Primidone (Mysoline)
Category D
Class: Clonazepam (Klonopin)
Benzodiazepine anticonvulsant (long-acting)
MOA: Clonazepam (Klonopin)
Binds to benzodiazepine receptors in CNS to enhance GABA activity -> inc Cl- influx -> inhibition of CNS synaptic transmission
Class: Phenytoin (Dilantin)
Anticonvulsant
MOA: Phenytoin (Dilantin)
Reduces Na and Ca and currents across neuronal membranes
Indication: Phenytoin (Dilantin)
Status epilepticus, focal (partial) seizures
Side effects: Phenytoin (Dilantin)
NYSTAGMUS, GINGIVAL HYPERPLASIA, ataxia, hepatotoxicity, possible BM suppression
Class: Carbamazepine (Tegretol)
Anticonvulsant
MOA: Carbamazepine (Tegretol)
Similar to phenytoin (reduction of Na, Ca currents)
Indication: Carbamazepine (Tegretol)
prophylaxis against all seizure types except absence
Contraindications: Carbamazepine (Tegretol)
Use with monoamine oxidase inhibitors (inc. risk for HTN crisis)
Class: Valproic acid (Depakote)
Anticonvulsant
Indication: Valproic acid (Depakote)
Generalized (tonic-clonic) seizures, bipolar do, chronic pain syndromes
Contraindications: Valproic acid (Depakote)
Pregnancy
Class: Ethosuximide (Zarontin)
Anticonvulsant
Indication: Ethosuximide (Zarontin)
Absence seizures, status epilepticus
MOA: Ethosuximide (Zarontin)
Possibly affects T-type Ca ion channels
Side effects: Ethosuximide (Zarontin)
HA, N, V, fatigue, ataxia, blurred vision, confusion, skin rashes, insomnia, GINGIVAL HYPERPLASIA, LUPUS-LIKE SYNDROME, hepatotoxicity
Class: Gabapentin (Neurontin)
Anticonvulsant, atypical analgesic
MOA: Gabapentin (Neurontin)
Appears to potentiate GABA and affects N-type Ca channels
Indication: Gabapentin (Neurontin)
Adjunctive tx for partial seizures, CHRONIC PAIN SYNDROMES (POST-HERPETIC NEURALGIA), migraines
Class: Lamotrigine (Lamactil)
Anticonvulsant
Indication: Lamotrigine (Lamactil)
Generalized (tonic-clonic) seizures
Class: Levetiracetam (Keppra)
Anticonvulsant
Indication: Levetiracetam (Keppra)
Generalized (tonic-clonic) seizures
The symptoms of Parkinson’s disease result from __
loss of dopamine-secreting cells in the pars compacta region of substantia nigra
What enzyme converts Levodopa into dopamine?
Dopa-decarboxylase
Levodopa is usually combined with a ___
peripheral dopa-decarboxylase inhibitor
MOA: peripheral dopa-carboxylase inhibitor
prevents Levadopa from being prematurely converted into dopamine in the adrenal glands
How long does treatment with Levodopa typically work?
Average of approximately 5 years
Contraindications: Levodopa and combinations
Use with MAO inhibitor b/c of hypertensive crisis
Use in patients with psychiatric conditions (bc worsening of psychotic sxs)
Use with dopamine-blocking antipsychotic agent
Class: L-dopa with Carbidopa (Sinemet)
Dopamine precursor with peripheral dopamine decarboxylase inhibitor
Indication: L-dopa with Carbidopa (Sinemet)
Parkinson’s disease
MOA: L-dopa with Carbidopa (Sinemet)
Increases dopamine levels in the brain, esp. in substantia nigra
Side effects: L-dopa with Carbidopa (Sinemet)
Hallucinations, nightmares, dyskinesias, serpentine-like movement (chorea)
Use of dopamine agonists (timing)
Often used early in tx so that L-dopa therapy can be delayed
Class: Bromocriptine (Parlodel)
Dopamine agonist
Indication: Bromocriptine (Parlodel)
Parkinson’s dz, PRL-secreting adenomas, acromegaly
MOA: Bromocriptine (Parlodel)
Mimics dopamine in stimulation of dopamine receptor sites
Crosses BBB
Class: Benzotropine (Cogentin)
Anticholinergic
Indication: Benzotropine (Cogentin)
Parkinson’s (esp. when tremor or drooling are prominent) - minimal efficacy as monotherapy
Diminish side effects of antipsychotic drugs
MOA: Benzotropine (Cogentin)
Anticholinergic antagonist at muscarinic receptor sites
MOA: Amantadine (Symmetrel)
Mb N-methyl-D-aspartate (NMDA) receptor antagonist -> dec. dopamine reuptake
Indications: Amantadine (Symmetrel)
Early PD (monotherapy) to delay L-dopa use
Adjunct in later PD (esp. in pts w/ levodopa-related dyskinesias
Influenza A
Class: Amantadine (Symmetrel)
Anti-Parkinson’s, anti-viral agent
Duration: Amantadine (Symmetrel)
Many pts experience diminished/absent response within 6 months or less
Parkinson’s tx options by efficacy (most-least)
L-dopa > Bromocriptine > Amantadine > anticholinergics
Class: Memantine (Namenda)
NMDA glutamate receptor antagonist
MOA: Memantine (Namenda)
NMDA receptor blockage -> inhibition of prolonged influx of Ca2+ ions, which play an imp. role in neuronal excitotoxicity
5HT3 receptor antagonist
dopamine D2 receptor agonist
Nicotinic ACh receptor antagonist
Indication: Memantine (Namenda)
Alzheimer’s disease
What class of drugs are postulated to play a role in the neurologic deficits associated w/ Alzheimer’s disease?
Anticholinergics
Class: Donepezil (Aricept)
Centrally-acting reversible acetylcholinesterase inhibitor
Indication: Donepezil (Aricept)
Alzheimer’s disease, Autism
What drug may potentially increase/improve vocab and expressive language of children with autism?
Donepezil (Aricept)
Class: Rivastigmine (Exelon)
Centrally-acting reversible acetylcholinesterase inhibitor
Indication: Rivastigmine (Exelon)
Mild-mod dementia dt Alzheimer’s
Mild-mod dementia dt PD
Younger onset dementia
Class: Galantamine (Razadyne)
Acetylcholinesterase inhibitor
Indication: Galantamine (Razadyne)
Mild-mod Alzheimer’s dz, vascular dementia
OD Sxs: Acetylcholinesterase inhibitor
N, V, salivation, sweating, bradycardia, hypotension, convulsions, circulatory collapse
Tx: Acetylcholinesterase inhibitor OD
Atropine
Drugs for focal (partial) seizures (3)
Phenytoin (Dilantin)
Phenobarbital (Phenobarb)
Primidone (Mysoline)
Drugs for absence (petit mal) seizures (1)
Ethosuximide (Zarontin)
Drugs for generalized (tonic-clonic) seizures (4)
Lamotrigine (Lamictal)
Levetiracetam (Keppra)
Topiramate (Topamax)
Valproate (Depakote)
What type of drugs are a first-line option for acute seizures, but not for long-term treatment?
Benzodiazepines (Diazepam, Clonazepam)
Drugs for status epilepticus (4)
Lorazepam (Ativan)
Diazepam (Valium)
Phenytoin (Dilantin)
Ethosuximide (Zarontin)
Indications: Lithium carbonate (Eskalith)
Bipolar d/o and manic episodes, schizophrenia