Drugs Flashcards
Levodopa
Dopaminergic Agent
Class: Dopamine (DA) precursor
MOA: Crosses BBB and is converted to dopamine–> improves nigrostriatal functioning
Given with carbidopa (as Sinemet);
Use: firstline treatment for Parkinson’s unless patient is young (want to delay as long as possible)
SE: Dyskinesias; hypotension, nausea, anxiety, fatigue
Psychoses of dosed too high
MAO-A inhibitors are contraindicated
(except MAO-B, which only hits DA)
Carbidopa
Dopaminergic Agent
Class: Aromatic amino acid decarboxylase inhibitor
MOA: Inhibits peripheral conversion of L-DOPA to dopamine; does not cross BBB
Use: Parkinson’s (given with Levadopa to
lower side effects)
SE: Dyskinesias, on-off phenomenon, —
MAO-A inhibitors are contraindicated
(except MAO-B, which only hits DA)
Buproprion
Dopaminergic Agent
Class: Norepinephrinedopamine reuptake inhibitor (NDRI)
MOA: Blocks dopamine transporter (DAT) ->
increased dopamine in synapse
Use: Parkinson’s (and depression, smoking cessation, weight loss)
SE: Insomnia, anxiety, agitation, nausea, dry mouth, sweating, palpitations, Mild increase in BP
dextroamphetamine
lisdexamfetamine
Dopaminergic Agent
Class: Stimulant
MOA: Blocks dopamine transporter (DAT); also increases VMAT2
Use: ADHD
Norepi and dopamine side effects; weight loss; addictive Psychosis at high doses
Modafinil; Armodafinil
Dopaminergic Agent
Stimulant
Increases histamine activity in the tuberomammilary nucleus; may block DAT
Fatigue due to narcolepsy, apnea, shiftwork disorder
SEs are Similar to, but less severe, than amphetamines, Addiction possible
Selegiline
Dopaminergic Agent
MAO-B inhibitor
Prevents breakdown of DA
Early Parkinson’s; depression
Hypotension, dizziness, insomnia, weight gain Nausea, vomiting
For depression it comes in a patch called EMSAM
Rasagiline
Dopaminergic Agent MAO-B inhibitor Prevents breakdown of DA Early Parkinson's Hypotension, dizziness, insomnia, weight gain Nausea, vomiting
Tranylcypromine
Isocarboxazid
Phenelzine
Dopaminergic Agent
MAOI
Irreversibly inhibit both MAO-A and MAO-B
Depression
Hypotension, dizziness, insomnia, weight gain
Hypertensive crisis (with tyramine-rich foods); serotonin syndrome (MAOI + SSRI)
Entacapone
Dopaminergic Agent COMT inhibitor Prevents breakdown of DA Parkinson's Nausea, fatigue DA side effects Short-acting (2 hours)
Tolcapone
Dopaminergic Agent COMT inhibitor Prevents breakdown of DA Parkinson's Nausea, fatigue; liver failure, DA side effects Use only if entacapone fails.
Bromocriptine
Dopaminergic Agent Ergot D2 receptor agonist Increases DA activity Mild Parkinson's; Restless Leg Syndrome hyperprolactinemia Mania, nausea, dizziness, fatigue Peripheral DA-like effects
Must be titrated slowly due to hypotension
Pramipexole ;
Ropinerole
Dopaminergic Agent Selective D2 receptor agonist Increases DA activity Mild Parkinson's; Restless Leg Syndrome Syndrome Mania, nausea, dizziness, fatigue Peripheral DA-like effects
Less effective with motor symptoms of PD
Apomorphine
Dopaminergic Agent
D2 receptor agonist
Increases DA activity
Mild Parkinson’s; Restless Legs Syndrome
Mania, nausea, dizziness, fatigue Peripheral DA effects
Injectable only; serotonin receptor antagonists contraindicated (e.g., ondansetron)
Aripiprazole
Dopaminergic Agent D2 & D3 receptor (partial) agonist I ncreases DA activity Schizophrenia; depression Less side effects than other DA agonists; akathisia
Amantadine
Dopaminergic Agent Anti-viral Stimulates D2 receptors, blocks DAT Mild Parkinson's (2nd-line); influenza Nausea, dizziness, psychosis, insomnia, seizures ---
Contraindicated in elderly with dementia (anticholinergic effects)
Reserpine
Dopaminergic Agent Synapse depleter Blocks VMAT (no release of monoamines into synapses) Use: Hypertension SE: Depression
Tetrabenazine
Dopaminergic Agent Synapse depleter Blocks VMAT (no release of monoamines into synapses) Huntington's Chorea, Depression is a SE
Benztropine;
Trihexiphenidyl
Dopaminergic Agent
Anticholinergics
Antagonize the ACh muscarinic receptor
Early Parkinson’s; reduce EPS parkinsonian side effects
Typical anticholinergic (dry mouth, blurred vision, racing heart, constipation, confusion, delirium, hallucinations)
Contraindicated in demented Parkinson’s; abrupt discontinuation exacerbates symptoms
Diphenhydramine
Dopaminergic Agent
Antihistamine Anticholinergic properties Reduce EPS Parkinsonian side effects
Typical anticholinergic (dry mouth, blurred vision, racing heart, constipation, confusion, delirium, hallucinations)
Chlorpromazine;
Thioridazine
Dopaminergic Agent
First-generation antipsychotics (Low Potency)
Non-selective D2 receptor antagonism
Use: Psychosis (schizophrenia)
SE: EPS; fatigue and weight gain (H1 antagonism); anticholinergic effects; orthostasis (alpha1 antagonism)
Tardive dyskinesia with chronic use
Little effect on negative symptoms of Schizophrenia
Fluphenazine;
Thiothixine ;
Haloperidol
Dopaminergic Agent
First-generation antipsychotics (High Potency)
Non-selective D2 receptor antagonism
Use: Psychosis (schizophrenia); movement disorder in Huntingtons
SE: EPS; NMS
Tardive dyskineasia with chronic use
Little effect on negative symptoms
Clozapine
Dopaminergic Agent
Second-Generation Antipsychotic
D2 (& D1, D4) receptor antagonist; 5HT2a receptor antagonist
Use: Refractory shizophrenia
Side effects similar to other “pines”,
but also agranulocytosis (NMDA receptor antagonism?)
Most metabolic risk of all
antipsychotics, but little EPS/TD;
must monitor WBC bc of agranulocytosis
Olanzapine ;
Quetiapine ;
Asenapine
Dopaminergic Agent Second-Generation Antipsychotics D2 receptor antagonist, 5HT2a receptor antagonist Use: Psychosis, mania, agression SE: Suicide risk in ages
Risperidone; Ziprazidone; Paliperidone; Iloperidone; Lurasidone
Dopaminergic Agent Class: Second-Generation Antipsychotics MOA: D2 receptor antagonist; but various other receptor agonism/antagonism Use: Psychosis, mania, agression SE: Suicide risk in ages
Pilocarpine HCl
Ocular Drug
Class: Direct muscarinic agonist
Use: Pupillary constriction, increased aqueous outflow
Treatment of glaucoma (both open angle and acute closed angle); cataract surgery
SE: Decreased vision when patient has cataracts due to miosis and headache, Bronchospasm, salivation, nausea, vomiting, diarrhea, abdominal pain, tenesmus, lacrimation, sweating
Used less frequently today due to side effects (SLUDGE)
Echothiophate
Ocular Drug Indirect muscarinic agonist Irreversibly binds cholinesterase Use: Treatment of glaucoma --- SE: Bronchospasm, salivation, nausea, vomiting, diarrhea, abdominal pain, tenesmus, lacrimation, sweating
Used less frequently today due to side effects
Atropine
Ocular Drug
Antimuscarinic
Pupillary dilatation; paralysis of ciliary body
Use: Improve discomfort during active eye inflammation (ueveitis)
SE: Ataxia, nystagmus, restlessness, mental confusion, hallucination, violent and aggressive behavior, insomnia, photophobia, urinary retention
Very long acting so not used unless severe inflammation
Scopolamine
Ocular Drug
Antimuscarinic
Pupillary dilatation; paralysis of ciliary body
Improve discomfort during active eye inflammation (ueveitis) (also used to treat motion sickness)
SE: Ataxia, nystagmus, restlessness, mental confusion, hallucination, violent and aggressive behavior, insomnia, photophobia, urinary retention
Tropicamide
Ocular Drug
Antimuscarinic
Pupillary dilatation; paralysis of ciliary body
Most commonly used cycloplegia for eye exams
SE: Ataxia, nystagmus, restlessness, mental confusion, hallucination, violent and aggressive behavior, insomnia, photophobia, urinary retention
Edrophonium
Ocular Drug
Nm agonist
Destroys acetylcholinesterase
Use: Diagnose myasthenia gravis
Epinephrine
Ocular Drug
Direct adrenergic agonist
Dilation of episcleral vessels –> increased aqueous outflow
SE: Extrasystoles, palpitation, hypertension, myocardial infarction, trembling, paleness, sweating
Hydroxyamphetamine
Ocular Drug
Class: Indirect adrenergic agonist
MOA: Release NE
Use: Separates 1st and 2nd from 3rd order neuron dysfunction in Horner’s syndrome; positive dilation means 1st or 2nd order, an ominous sign
Cocaine
Ocular Drug
Indirect adrenergic agonist
Prevent reuptake of NE
Use initially to confirm diagnosis of Horner’s Syndrome
Phenylephrine
Ocular Drug
Direct α1-agonist —
Use: Dilate pupil for eye exam and cataract surgery —
Extrasystoles, palpitation, hypertension, myocardial infarction, trembling, paleness, sweating
Caution in elderly patients: at 10% can cause cardiac side effects
Brimondine tartrate
Direct α2-agonist Suppresses aqueous humor production through action of cAMP in non-pigmented ciliary epithelium Primary agent for treatment of glaucoma --- --- May cause follicular conjunctivitis; use with MAOi can cause fatigue/drowsiness
Timolol
Ocular Drug
β-blocker
Reduce intraocular pressure by reducing aqueous production at the ciliary process
Use: Second line treatment of glaucoma —
Bradycardia, hypotension, syncope, palpitation, congestive heart failure, bronchospasm, mental confusion, depression, fatigue, lightheadedness, hallucinations, memory impairment, sexual dysfunction, hyperkalemia
Contraindicated in CHF, asthma; bradycardia over time may produce tachyphylaxis
Levobunolol
Ocular Drug
β-blocker
Reduce intraocular pressure by reducing aqueous production at the ciliary process
Use: Second line treatment of glaucoma —
Bradycardia, hypotension, syncope, palpitation, congestive heart failure, bronchospasm, mental confusion, depression, fatigue, lightheadedness, hallucinations, memory impairment, sexual dysfunction, hyperkalemia
Betaxolol
β1-blocker
Reduce intraocular pressure by reducing
aqueous production at the ciliary process Second line treatment of glaucoma
Latanoprast
Prostaglandin analog Increase uveoscleral outflow Primary agent for treatment of glaucoma Eyelash growth, change in iris color, intraocular inflammation May cause cystoid macular edema in cataract surgery and activate herpes
Travoprost
Prostaglandin analog Increase uveoscleral outflow Primary agent for treatment of glaucoma Eyelash growth, change in iris color
May cause cystoid macular edema in
cataract surgery; more effective in
African Americans
Bimatoprost
Prostaglandin analog Increase uveoscleral outflow Primary agent for treatment of glaucoma Eyelash growth, change in iris color
May cause cystoid macular edema in
cataract surgery and activate herpes
Unoprostone isopryl
Prostaglandin analog Increase uveoscleral outflow Glaucoma Eyelash growth, change in iris color Least effective overall
Nifedipine
Ca-channel blocker Increases ocular perfusion at nervehead Low-tension glaucoma Not widely used.
Dorzolamide HCl
Carbonic anhydrase
inhibitor
Reduce aqueous production via interfere
with the active transport of Na through Na-
K-ATPase pump Second line glaucoma therapy Red eyes, lid allergies
Contraindicated in sulfonamide
allergies
Acetazolamide
Carbonic anhydrase inhibitor Reduce aqueous production via interfere with the active transport of Na through Na- K-ATPase pump Oral agent used for advanced glaucoma and with cataract surgery Paresthesia, fatigue, drowsiness, depression, diarrhea, metaboliv acidosis, electrolyte changes Anaphylaxis, blood dyscrasias Used only if other topical therapy fails.
Brinzolamide
Carbonic anhydrase
inhibitor
Reduce aqueous production via interfere
with the active transport of Na through Na-
K-ATPase pump Second line glaucoma therapy Red eyes, lid allergies
Tranylcypromine;
Phenelzine
Antidepressant
Class: MAOI
MOA: Irreversibly inhibit both MAOa and MAOb
Use: Depression, anxiety, PTSD, chronic pain, enuresis, bulimia, alcoholism
Hypertensive crisis (with tyraminerich foods); serotonin syndrome (MAOI + SSRI); agitation (rare), delerium --> seizures Anticholinergic, orthostatic hypotension, sexual dysfunction, weight gain, sedation
Desipramine;
Imipramine;
Amitriptyline;
Nortriptyline
Tricyclic Antidepressant
Block reuptake of NE or 5-HT at varying potencies and selectivity; also variably block muscarinic, a-adrenergic, dopamine, and histamine receptors
Depression, anxiety, PTSD, chronic pain, enuresis, bulimia, alcoholism
Sympathomimetic (cardiac arrhythmias and conduction defects, especially at OD)
Antimuscarinic, orthostatic hypotension, sedation (additive
with alcohol), seizures
Not very safe; rarely used anymore
Fluoxetine; Paroxetine
SSRI
Inhibit reuptake of 5-HT (and NE to lesser extent)
Depression, anxiety, PTSD, chronic pain, enuresis, bulimia, alcoholism; premenstrual dystrophic disorder
Serotonin syndrom (with MAOIs)
Fewer than tricyclics; mostly nausea, decreased sexual
function
Fluoxetine and Paroxetine are Potent P450 inhibitors;
Fluoxetine forms active metabolite (norfluoxetine)
Paroxetine
SSRI
Inhibit reuptake of 5-HT (and NE to lesser extent)
Depression, anxiety, PTSD, chronic
pain, enuresis, bulimia, alcoholism Serotonin syndrom (with MAOIs)
Fewer than tricyclics; mostly
nausea, decreased sexual
function Potent P450 inhibitor
Sertraline
SSRI Inhibit reuptake of 5-HT (and NE to lesser extent) Depression, anxiety, PTSD, chronic pain, enuresis, bulimia, alcoholism Serotonin syndrom (with MAOIs) Fewer than tricyclics; mostly nausea, decreased sexual functio
Escitalopram
SSRI Inhibit reuptake of 5-HT (and NE to lesser extent) Depression, anxiety, PTSD, chronic pain, enuresis, bulimia, alcoholism Serotonin syndrom (with MAOIs) Fewer than tricyclics; mostly nausea, decreased sexual function
Citalopram
SSRI Inhibit reuptake of 5-HT (and NE to lesser extent) Depression, anxiety, PTSD, chronic pain, enuresis, bulimia, alcoholism Serotonin syndrom (with MAOIs) Fewer than tricyclics; mostly nausea, decreased sexual function
Duloxetine
SNRI Inhibits reuptake of 5-HT and NE
Depression, anxiety, PTSD, chronic
pain, enuresis, bulimia, alcoholism
Venlafaxine
SNRI Inhibits reuptake of 5-HT and NE
Depression, anxiety, PTSD, chronic
pain, enuresis, bulimia, alcoholism
Bupropion
Atypical Blocks DA and NE reuptake Depression, anxiety, PTSD, chronic pain, enuresis, bulimia, alcoholism; maintain nicotine abstinence in quitting smokers Lowers seizure threshold
Mirtazapine
Atypical 5HT2a antagonists; also inhibit 5HT reuptake Depression, anxiety, PTSD, chronic pain, enuresis, bulimia, alcoholism
Lithium
Unknown; lithium depletes secondary messengers IP3 and DAG, important in aadrenergic and muscarinic-cholinergic transmission Anti-manic/mood-stabilizing (bipolar); long-term cluster headache prevention If elevated levels: neurotoxicity, cardiac toxicity, renal dysfunction Drowsiness, weight gain, tremor, polydipsia, polyuria Nausea and vomiting early sign of lithium OD; indomethacin and Nadepleting diuretics should be avoided (increase [Li])
Nalmefene
Opiod antagonist — —
May produce a prolonged
withdrawal state (nausea, vomiting,
piloerection, yawning)
N-acetylcysteine
Antioxidant
Supplies sulfhydryl groups to glutathione;
improves microcirculation, provides antiinflammatory
effect Acetaminophen overdose
Fomepizole
Blocks alcohol dehydrogenase Methanol & ethylene glycol poisoning — — Very expensive
Cocaine
CNS stimulant Blocks reuptake of dopamine, norepinephrine, and serotonin Topical anesthetic, combined vasoconstrictor and local anesthetic Sympathetic effects; paranoia, aggression --- Rapidly hydrolyzed by plasma cholinesterase; crack is the free base form
LSD
Schedule I Hallucinogen Agonist at 5HT2A receptors on Raphe cell body --> inhibition of Raphe Nuclei firing --> increased sensory input; partial dopamine agonist Schedule I hallucinogen; model hallucinogen against which all others compared; limited studies in psychoanalysis, alcoholism, autistic children, and terminal cancer patients Bad trips (anxiety attack, panic attack), flashbacks, "street drug" lifestyle; no overdoses, birth defects, or chronic psychoses linked to LSD --- Oxidized in liver; cross tolerance with mescaline and psilocybin
Mescaline
Schedule I Hallucinogen Agonist at 5HT2A receptors on Raphe cell body --> inhibition of Raphe Nuclei firing --> increased sensory input; partial dopamine agonist --- --- Cross tolerance with LSD and psilocybin
Psilocybin
Schedule I Hallucinogen Agonist at 5HT2A receptors on Raphe cell body --> inhibition of Raphe Nuclei firing --> increased sensory input; partial dopamine agonist --- --- --- Cross tolerance with mescaline and LSD
