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Common adverse effect of antipsychotics, MPTP (contaminant in illicit meperidine analog), and cholinergic excess

Drug-induced Parkinsonism

Precursor of dopamine that can cross the blood-brain-barrier and used to alleviate motor dysfunction in Parkinson's disease

Levodopa (L-dopa)

Inhibits peripheral DOPA decarboxylase, reduces peripheral side effects of dopamine precursor and enhances its delivery to the brain

Carbidopa

Two fluctuations in clinical response associated with long-term use of dopamine precursor

"Wearing off" and "on-off phenomenon"

Monoamine oxidase type B (MAO-B) inhibitors; used as monotherapy for early or mild Parkinson's disease or adjunct to improve motor function (2)

Selegiline, rasagiline

Catechol-O-methyltransferase (COMT) inhibitors; used as adjunct to improve motor function in Parkinson's patients (2)

Entacapone, tolcapone

Ergot D2 agonist; used as adjunct to improve motor function in Parkinson's patients

Bromocriptine

Non ergot D2 agonists; used for Parkinson's and Restless Legs Syndrome (2)

Pramipexole, ropinirole

An antiviral that enhances dopamine release from nigrostriatal neurons

Amantadine

Centrally-acting anticholinergic; used for tremor and rigidity, little effect on bradykinesia in patients with Parkinson's

Benztropine

Drug of choice indicated for familial or essential tremors

Propranolol

Vesicle monoamine transporter inhibitors; used for Huntington's disease (2)

Tetrabenazine, reserpine

An antipsychotic with dopamine receptor antagonist activity used for Huntington's disease

Haloperidol

Centrally-acting cholinesterase inhibitors used for Alzheimer's (3)

Donepezil, rivastigmine, galantamine

Noncompetitive antagonist of NMDA receptors used for Alzheimer's

Memantine

Main classes of CNS depressant drugs of abuse (3)

Alcohol, opioid, barbiturate/benzodiazepine

Agent that is metabolized by alcohol dehydrogenase or microsomal ethanol-oxidizing system (MEOS) to acetaldehyde; displays zero-order kinetics of elimination

Ethanol

Enzyme that is induced through chronic exposure to alcohol, may contribute to tolerance

Microsomal ethanol oxidizing system (MEOS)

Complications of the gastrointestinal system associated with chronic alcohol use (4)

Mallory-Weiss syndrome, hepatitis, cirrhosis, pancreatitis

Neurological abnormality caused by chronic alcohol use and thiamine deficiency

Wernicke-Korsakoff Syndrome

Most common neurologic abnormality in chronic alcoholics

Neurologic deficits (peripheral neuropathy)

Life-threatening alcohol withdrawal syndrome that peaks at 5 days after the last drink

Delirium tremens

Aldehyde dehydrogenase inhibitor; used as deterrent for alcohol use

Disulfiram

Opioid receptor antagonist; used to prevent alcohol abuse

Naltrexone

Competes for alcohol dehydrogenase and is used in methanol or ethylene glycol poisoning (2)

Fomepizole, ethanol

Most commonly abused opioids (3)

Heroin, morphine, oxycodone

Respiratory and CNS depression, pinpoint pupils, seizures, and needle track marks are symptoms of this intoxication

Opioid

Opioid receptor antagonist that is used to treat opioid intoxication, may cause more rapid and intense symptoms of withdrawal

Naloxone

Sweating, dilated pupils, piloerection, and flu-like symptoms are symptoms of withdrawal from this class of drugs

Opioids

Opioids used for long-term maintenance from opioid withdrawal (2)

Methadone, buprenorphine

Most widely abused sedative hypnotics

Short-acting barbiturates (pentobarbital)

Date rape drugs that work through enhancement of GABA receptors in the brain (2)

Flunitrazepam, GHB (γ-hydroxybutyrate)

Benzodiazepine antagonist used to treat benzodiazepine intoxication

Flumazenil

Major CNS stimulant drugs of abuse (4)

Caffeine, nicotine, cocaine, amphetamines

Treatments available for nicotine addiction (5)

Patch, gum, lozenge, bupropion, varenicline

CNS stimulant that acts by inhibiting reuptake of neurotransmitters; may cause pupil dilation, alter tactile sensation, irregular breathing, and cardiac toxicity

Cocaine

Amphetamine derivatives commonly abused (2)

Methamphetamine (crystal meth), MDMA (methylenedioxymeth-amphetamine, or ecstasy)

Drug of abuse that was developed as a dissociative anesthetic; intoxication leads to both horizontal and vertical nystagmus, analgesia, psychosis, delirium, and seizures

PCP (phencyclidine, angel dust)

Synthetic ergot derivative that can produce perceptual hallucinations and used as an illicit drug; may cause paranoia

LSD (lysergic acid diethylamide)

Active ingredient is tetrahydrocannabinol (THC); adverse effects include impairment of judgment, altered sense of time, increased appetite, and hallucinations

Marijuana

Use of all antipsychotic medication in this group of patients is associated with increased risk of deaths

Elderly with dementia-related psychosis

Antipsychotic class that represses primarily the positive symptoms of schizophrenia

Typical antipsychotics

Primary mechanism of action of typical antipsychotics

Inhibits D2 receptors

Common endocrine adverse effects of all typical antipsychotic drugs

Hyperprolactinemia, galactorrhea

Low potency, typical antipsychotic drugs (2)

Chlorpromazine, thioridazine

Typical antipsychotic associated with retinopathy and cardiac toxicity

Thioridazine

Common adverse effects of low potency typical antipsychotic drugs (3)

Dry mouth (anticholinergic), sedation (antihistamine), hypotension (α1 block)

High potency, typical antipsychotic drugs (3)

Haloperidol, fluphenazine, trifluoperazine

Typical antipsychotic that can also be used for Tourette syndrome

Haloperidol

Adverse effects more commonly associated with high potency typical antipsychotic drugs (4)

Dystonia, akathisia, bradykinesia, tardive dyskinesia (extrapyramidal symptoms)

Treatment for drug-induced acute extrapyramidal symptoms (2)

Benztropine, diphenhydramine

Life-threatening adverse effect associated with typical antipsychotic drugs

Neuroleptic malignant syndrome

Treatment for drug-induced neuroleptic malignant syndrome

Dantrolene

Advantage of atypical over typical antipsychotics

Less extrapyramidal symptoms, more effect against negative symptoms of schizophrenia

Primary mechanism of action of atypical antipsychotics

Inhibit 5-HT2 receptors

Atypical antipsychotic that can produce potentially fatal agranulocytosis and increase incidence of seizures

Clozapine

Atypical antipsychotics that can cause weight gain (2)

Clozapine, olanzapine

Atypical antipsychotics that can prolong the QT interval (2)

Risperidone, ziprasidone

Atypical antipsychotic that can increase prolactin levels and cause gynecomastia and irregular menstruation in men and women, respectively

Risperidone

Atypical antipsychotic that can also be used to treat irritability in autistic children

Aripiprazole

tricyclic antidepressants

-iptyline, -ipramine, doxepin, amoxapine

Mechanism of action of tricyclic antidepressants

Block serotonin and norepinephrine reuptake

Common adverse effects of tricyclic antidepressants

Autonomic (block muscarinic and alpha 1), sedation

Tricyclic secondary amines that produce less sedation and autonomic adverse effects (compared with tricyclic tertiary amines) (2)

Nortriptyline, desipramine

Life-threatening adverse effects associated with tricyclic antidepressants (3)

Convulsion, cardiotoxicity, coma (3 C's)

Tricyclic antidepressant used for enuresis

imipramine

Tricyclic antidepressant used in obsessive compulsive disorder

Clomipramine

Tricyclic antidepressant with antihistamine effect and is indicated for insomnia

Doxepin

Class of antidepressants that has fewer sedative and autonomic adverse effects than tricyclic antidepressants and indicated for panic disorder, generalized anxiety disorder, social phobias, bulimia, obsessive compulsive behavior, and post-traumatic stress disorder

Selective serotonin reuptake inhibitors (SSRI)

Selective serotonin reuptake inhibitors (4)

Fluoxetine, paroxetine, sertraline, citalopram

Serious adverse effect of selective serotonin reuptake inhibitors when used with other drugs such as monoamine oxidase inhibitors, serotonin-norepinephrine reuptake inhibitors, or tricyclic antidepressants

Serotonin Syndrome

Selective serotonin-norepinephrine reuptake inhibitors (2)

Duloxetine, venlafaxine

Class of drugs that is most useful in patients with anxiety, hypochondriasis, and depression that is refractory to other antidepressants

Monoamine oxidase inhibitors

Mechanism of action of isocarboxazid, phenelzine, and tranylcypromine

Irreversible inhibition of monoamine oxidase A and B

Mechanism of action of selegiline

Selectively inhibits monoamine oxidase B

A fatal condition that results from combination of monoamine oxidase inhibitors with tyramine-containing foods

Hypertensive crisis

Antidepressant that non-selectively inhibits neuronal reuptake; less likely to cause sedation, autonomic, cardiovascular, or sexual dysfunction; also used for smoking cessation

Bupropion

Antidepressant that inhibits serotonin reuptake but also antagonizes 5HT-2 receptors; causes priapism

Trazodone

Antidepressant that inhibits alpha 2, 5HT-2, and 5HT-3 receptors to increase release of norepinephrine and serotonin

Mirtazapine

First line drug for classic bipolar disorder with euphoric mania

Lithium

Major route of elimination for Lithium

kidneys

Adverse effects of lithium (4)

Tremor, hypothyroidism, nephrogenic diabetes insipidus, fetal cardiac defects

Ganglion blockers used in research; high affinity for neuronal nicotinic receptors (2)

Hexamethonium, trimethaphan

Direct-acting cholinomimetics that increase aqueous outflow through ciliary muscle contraction and opening of trabecular meshwork (2)

Pilocarpine, carbachol

Indirect-acting cholinomimetics that increase aqueous outflow through ciliary muscle contraction and opening of trabecular meshwork (2)

Physostigmine, echothiophate

Nonselective alpha agonist that decreases aqueous production

Epinephrine

Selective alpha 2 agonist that decreases aqueous production

Brimonidine

Beta blockers that decrease aqueous production (3)

Timolol (nonselective), betaxolol (selective), carteolol (nonselective)

Carbonic anhydrase inhibitor used to decrease aqueous humor production

Acetazolamide

Prostaglandin E2 alpha analog used to increase aqueous humor outflow

Latanoprost

Common adverse effect of sedative hypnotics

CNS depression

Mechanism of action of benzodiazepines

Increase frequency of GABA-mediated chloride ion channel (GABAA) opening

Main route of metabolism for benzodiazepines

hepatic

Useful adverse effect of benzodiazepines in patients undergoing stressful procedures or surgery

Anterograde amnesia

Benzodiazepines that are metabolized only by Phase II conjugation and therefore is useful in elderly patients (3)

Lorazepam, oxazepam, and temazepam

Benzodiazepines that have active metabolites with long half-lives (2)

Diazepam, chlordiazepoxide

Clinical uses of benzodiazepines (5)

Anxiety, insomnia, alcohol detoxification, status epilepticus, spasticity

Reason why benzodiazepines are safer than barbiturates

Benzodiazepines do not directly activate GABA-A

Mechanism of action of barbiturates

Increase duration of GABAA chloride channel opening

Most serious adverse effects of barbiturates (2)

Respiratory and cardiovascular depression