Pharmacology One-Liners 2 Flashcards
First-line drugs for acute gout
Indomethacin, naproxen
NSAID avoided in gout because low doses increase uric acid levels
Aspirin
Mechanism of action of colchicine
Inhibits microtubules assembly, decreases leukocyte migration, and phagocytosis
Side effects of colchicine
Diarhhea, liver toxicity, myelosuppression
Agents that inhibit xanthine oxidases and used to treat chronic gout
Allopurinol, febuxostat
Recombinant uricase that enhances uric acid metabolism and indicated for gout refractory to conventional therapy
Pegloticase
DMARDs are slow-acting drugs for this indication
Rheumatic diseases
1st line for rheumatic arthritis for most patients
Low-dose methotrexate
Dose-limiting toxicity of methotrexate
Myelosuppression
A mixture of two agents with one agent active for rheumatic disease and the other for inflammatory bowel disease
Sulfasalzine
Agent used to treat chronic gout by increasing uric acid excretion through inhibition of URAT1 anion transporter
Probenecid
Alternative to methotrexate as 1st line for rheumatoid arthritis through inhibition of dihydroorotate dehydrogenase, which leads to decreased pyrimidine synthesis
Leflunomide
Side effect of penicillamine
Hypersensitivity (rash), nephrotoxicity, myopathy, myelosuppression
Anti-malarial drug used in rheumatoid arthritis
Hydroxychloroquine
Side effect of hydroxychloroquine
Retinopathy
Two drugs that bind and prevent action of tumor necrosis factor alpha (TNF-alpha)
Infliximab and etanercept
Neuromuscular blocking drugs
Structurally related to acetylcholine, used to produce muscle paralysis in order to facilitate surgery or artificial ventilation. Full doses lead to respiratory paralysis and require ventilation
Class of agents that block acetylcholine receptors at motor endplates and its effects can be reversed by cholinesterase inhibitors
Nondepolarizing blockers
Tubocurarine
Non-depolarizing neuromuscular blocker with long duration of action and is most likely to cause histamine release
Two non-depolarizing blockers that undergo Hofmann elimination, which is useful for patients with renal and hepatic deficiency
Atracurium, cisatracurium
Pancuronium
Non-depolarizing neuromuscular blocker with long duration of action that can block muscarinic receptor in the heart
These drugs strongly potentiate and prolong effect of neuromuscular blockers
Inhalation anesthetics (isoflurane), antibiotics (aminoglycosides, tetracyclines)
Succinylcholine
Depolarizing blocker that causes muscle relaxation and paralysis and can cause postoperative muscle pain
Two life-threatening side effects of succinylcholine
Hyperkalemia, malignant hyperthermia
Dantrolene
Drug for treating malignant hyperthermia associated with drug-drug interaction between halogenated anesthetics and depolarizing blocker
During Phase I depolarizing block this class of agents enhance muscle paralysis, but during Phase II block they may reverse muscle paralysis
Cholinesterase inhibitors
Neostigmine
Drug of choice for reversal of non-depolarizing neuromuscular blockade
Mechanism of action of cromolyn
Prevent mast cell degranulation (by blocking opening of Cl- channels)
Which enzyme does theophylline inhibit?
Phosphodiesterase
Somatropin
Growth hormone analog used in growth hormone deficiency
Octreotide
Somatostatin analog used for acromegaly, carcinoid, glucagonoma, and other growth hormone-producing pituitary tumors
Leuprolide
Gonadotropin-releasing hormone analog used for infertility (pulsatile administration) or suppression of gonadotropin production (continuous administration)
Ganirelix
Competitive antagonists at gonadotropin releasing hormone receptors used to prevent LH surger during controlled ovarian hyperstimulation
Bromocriptine
Ergot dopamine agonist used to suppress prolactin release
Cosyntropin
Synthetic human corticotropin used for diagnosis of adrenal insufficiency
Oxytocin
Agent used to stimulate uterine contraction and labor, milk letdowns, and control postpartum bleeding
Levothyroxine (T4)
Agent of choice for the treatment of hypothyroidism
Liothyronine (T3)
An isomer of T3 which may be used in myxedema coma
Thioamide agents used in hyperthyroidism
Methimazole and propylthiouracil (PTU)
Thioamide less likely to cross placenta, inhibits peripheral conversion of T4 to T3 in high doses, and indicated for pregnant women in 1st trimester
Propylthiouracil (PTU)
Propylthiouracil mechanism of action
Inhibits thyroid peroxidase
Can be effective for short term therapy of thyroid storm, but after several weeks of therapy causes an exacerbation of hyperthyroidism
Iodide salts (potassium iodide)
Radioactive iodine
Permanently cures thyrotoxicosis, patients will need thyroid replacement therapy thereafter. Contraindicated in pregnancy
Used for symptomatic treatment of thyrotoxicosis by blocking cardiac adverse effects
Beta-blockers such as propranolol and esmolol
Glucocorticoids
Used for Addison’s disease, congenital adrenal hyperplasia inflammation, immune suppresion, and asthma
Two short-acting glucocorticoids
Hydrocortisone (cortisol), cortisone
Four intermediate-acting glucocorticoids
Prednisone, prednisolone, methylprednisolone, and triamcinolone
Two long-acting glucocorticoids
Betamethasone, dexamethasone
Two glucocorticoids with mineralocorticoid action
Fludrocortisone and deoxycorticosterone
Side effects of corticosteroids
Iatrogenic Cushing’s syndrome, hyperglycemia, impaired wound healing, osteoporosis, peptic ulcers, myopathy, adrenal suppression (>2 week treatment)
Aminoglutethimide
Inhibits conversion of cholesterol to pregnenolone therefore inhibiting corticosteroid synthesis
Ketoconazole
Antifungal agent used to inhibit adrenal and gonadal steroid synthesis
Metyrapone
Seelctive inhibitor of 11-hydroxylation and interferes with cortisol and corticosterone synthesis; used for adrenal function tests and is the only adrenal-inhibiting medication that can be administered to pregnant women with Cushing’s syndrome
Mifepristone (RU486)
Glucocorticoid receptor antagonist that is used as an abortifacient due to its strong antiprogestin activity
Three rapid-acting insulin used for postprandial glycemia
Aspart, lispro, glulisine
Short-acting insulin used intravenously for ketoacidosis
Regular insulin
Intermediate-acting insulin with variable pharmacokinetics; use is mostly replaced by long-acting insulin
Neutral protamine Hagedorn (NPH) insulin
Two long-acting insulin preparations that provide basal glycemia control
Glargine, detemir
Major side-effect of insulin
Hypoglycemia
Tolbutamide
First generation sulfonylurea that is safest for elderly diabetics due to its short half-life
Chlorpropamide
First generation sulfonylurea contraindicated in elderly diabetics because of very long half-life
Three second generation sulfonylureas
Glyburide, glipizide, glimepride
Mechanism of action of sulfonylureas
Close K+ channels, depolarize cell, open voltage-gated Ca2+ channels, release insulin
Common side effect of first-generation sulfonylureas
Disulfiram-like reactions with alcohol use
Common side effect of second-generation sulofnylureas
Hypoglycemia
Repaglinide
A meglitinide insulin secretagogue that has no sulfur in its structure and may be used in type 2 diabetics with sulfonylurea allergy
Nateglinide
A D-phenylalanine derivative insulin secretagogue that is useful for type 2 diabetics with very reduced renal function
Mechanism of action of repaglinide and nateglinide
Close K+ channels, depolarize cell, open voltage-gated Ca2+ channels, release insulin
First line drug used for treatment of Type 2 diabetes
Metformin
Mechanism of action of metformin
decreased gluconeogeesnis, increased peripheral glucose uptake; increase insulin sensitivity
Most serious side effect of metformin
Lactic acidosis
Two thiazolidinediones
Pioglitazone, rosiglitazone
Mechanism of action of thiazolidinediones
Activate PPAR-gamma, increased transcription of insulin-responsive genes, increased GLUT4 glucose transporter, increased insulin sensitivity
Side effect of thiazolidinediones
Weight gain, edema, heart failure, hepatotoxicity
Two alpha-glucosidase inhibitors
Acarbose, miglitol
Mechanism of action of alpha-glucosidase inhibitors
Act on intestine, delay digestion and absorption of glucose
Side effect of alpha-glucosidase inhibitors
Flatulence, diarrhea, abdominal cramps
Pramlintide
Amylin analog that delays gastric emptying and suppresses glucagon release
Two glucagon-like polypeptide-1 (GLP-1) analogs that increase insulin secretion and suppress postprandial glucagon release
Exenatide, liraglutide
Three dipeptidyl peptidase-4 (DPP-4) inhibitors that reduce breakdown of glucagon-like polypeptide-1, resulting in increased insulin secretion and suppress postprandial glucagon release
Sitagliptin, saxagliptin, linagliptin
Bisphosphonates
Alendronate and -dronates
Mechanism of action of bisphosphonates
Inhibits osteoclast activity and prevent bone resorption
Uses of bisphosphonates
Osteoporosis, Paget’s disease, hypercalcemia
Major side effects of bisphosphonates
Corrosive esophagitis, osteonecrosis of the jaw
Etidronate
First generation bisphosphonate when used long-term causes osteomalacia
May be used intranasally to decrease bone resorption
Calcitonin (salmon prep)
Vitamin given with calcium to ensure proper absorption
Vitamin D
Its use can increase risk of endometrial and breast cancer, cause postmenopausal uterine bleeding, but can stabilize bone mineral loss
Estrogen
Antiestrogen drug used for treatment of infertility in anovulatory women
Clomiphene
Tamoxifen
Selective estrogen receptor modulator most commonly used for treatment of breast cancer
Raloxifine
Selective estrogen receptor modulator used for prevention of osteoporosis and invasive breast cancer
Common side effect of tamoxifen and clomiphene
Hot flushes
Two estradiol derivatives with higher oral bioavailability and longer half-lives that are primarily used as oral contraceptives
Ethinyl estradiol and mestranol
Testosterone
Androgen receptor agonist used to treat hypogonadism and promote secondary sex characteristics
Finasteride
5 alpha-reductase inhibitor used for benign prostatic hyperplasia and male patter baldness
Danazol
Partial androgen agonist used for endometriosis and hereditary angioedema
Flutamide
Androgen receptor antagonist used to treat prostate cancer
Cyproterone
Androgen receptor antagonist used for hirsutism in females
Autacoids
A class of endogenous substances that include histamine, serotonin, prostaglandins, vasoactive peptides that work in autocrine or paracrine manner
Two peptides that increase capillary permeability and edema
Bradykinin and histamine
Distribution of H1 histamine receptors
Smooth muscle and mast cells
Distribution of H2 histamine receptors
Stomach, heart, and mast cells
Distribution of H3 histamine receptors
Nerve endings, CNS
Most common side effect of 1st generation antihistamines
Sedation, anticholinergic
Dephenhydramine
1st generation antihistamine that is highly sedating
Chlorpheniramine
1st generation antihistamine that is least sedating
Major indication for H1 antihistamines
IgE mediated allergic reaction (allergic rhinitis, urticaria)
Antihistamine that is indicated for allergies, motion sickness, and insomnia
Diphenhydramine
Antihistamine with motion sickness as the only indication
Dimenhydrinate
Three 2nd generation antihistamines
Fexofenadine, loratadine, and cetirizine
H2 antagonist that causes the most interactions with other drugs
Cimetidine
Indication for H2 antagonists
Acid reflux disease, duodenal ulcer and peptic ulcer disease
Location of serotonin type-1 (5HT-1) receptors
Mostly in the brain
Buspirone
5HT-1A receptor partial agonist indicated for generalized anxiety disorder; due to longer onset of action, is less effective for acute anxiety
5HT-1D/1B agonist used for migraine headaches
Sumatriptan and -triptans
Ergotaimne
Ergot alkaloid indicated for migraine headaches
Reason ergot alkaloids are contraindicated in pregnancy
Uterine contractions
Two side effects of ergot alkaloids
Prolonged vasospasm and hallucinations resembling psychosis
Two drugs that may be used off-label for ischemia and gangrene caused by ergot alkaloids overuse
Nitroprusside, nitroglycerin
Serotonin receptor responsible for serotonin syndrome
5HT2
H1 antihistamine with 5HT2 antagonist activity that is mostly used for carcinoid tumor but may be used to treat serotonin syndrome
Cyproheptadine
Location of serotonin type-3 (5HT-3) receptors
GI tract, vomiting center of medulla
5HT-3 antagonist used for the prevention of chemotherapy-induced nausea and vomiting
Ondansetron and -setrons
Ganglion blockers that were indicated (but not anymore) for severe hypertension
Hexamethonium, trimethaphan
Two direct-acting cholinomimetics that increase aqueous outflow through ciliary muscle contraction and opening of trabecular meshwork
Pilocarpine, carbachol
Two indirect-acting cholinomimetics that increase aqueous outflow through ciliary muscle contraction and opening of trabecular meshwork
Physostigmine, echothiophate
Nonselective alpha agonist that decreases aqueous production
Epinephrine
Selective alpha 2 agonits that decreases aqueous production
Brimonidine
Three beta blockers that decrease aqueous production
Timolol (nonselective)
Betaxolol (selective)
Carteolol (nonselective)
Carbonic anhydrase inhibitor used to decrease aqueous humor production
Acetazolamide
Prostaglandin 2 alpha analog used to increase aqueous humor outflow
Latanoprost
Common side effect of sedative hypnotics
CNS depression
Occurs when sedative hypnotics are used long-term
Tolerance and physical dependence
Mechanism of action of benzodiazepines
Increase frequency of GABA-mediated chloride ion channel (GABAa) opening
Main route of metabolism for benzodiazepines
Hepatic
Useful side effect of benzodiazepines in patients undergoing stressful procedures or surgery
Anterograde amnesia
Three benzodiazepines that are metabolized only by Phase II conjugation and therefor is useful in elderly patients
Lorazepam, oxazepam, temazepam
Two benzodiazepines that have active metabolites with long half-lives
Diazepam, chlordiazepoxide
Clinical uses of benzodiazepines
Anxiety, insomnia, alcohol detoxification, status epilepticus, spasticity
Reason why benzodiazepines are safer than barbiturates
Benzodiazepines work only in presence of GABA
Mechanism of action of barbiturates
Increased duration of GABAa chloride channel opening
Most serious side effect of barbiturates
Respiratory and cardiovascular depression
Barbiturates may precipitate this hematologic condition
Porphyria
Barbiturates decrease the effectiveness of many other drugs via this pharmacokinetic property
Induce CYP450
Effect of benzodiazepines and barbiturates on sleep architecture
Suppress REM
Three nonbenzodiazepine hypnotics that lack suppressive effect on REM and are preferred over benzodiazepines for the treatment of insomnia
Zolpidem, zaleplon, eszopiclone
Mechanism of action of zolpidem
Activates BZ1 subtype of GABAa receptor
Drug of choice for treatment of acute status epilepticus
Diazepam, lorazepam
Drug of choice for partial seizures
Carbamazepine
Antiepileptic drug used as first line for trigeminal neuralgia
Carbamazepine
Antiepileptic drug that can induce CYP450, is teratogenic, and can cause diplopia, ataxia, and blood dyscrasias; follows first order kinetics of eliminations
Carbamazepine
Drug of choice for generalized tonic-clonic seizures
Carbamazepine, phenytoin, valproic acid
Mechanism of action of phenytoin, carbamazepine, lamotrigine
Blocks sodium channels
Antiepileptic agent that exhibits zero-order kinetics, causes fetal hydantoin syndrome, and induces CYP450
Phenytoin
Side effects of phenytoin
Gingival hyperplasia, nystagmus, diplopia, and ataxia
Mechanism of valproic acid
Blocks sodium channels, T-type calcium channels, and increase GABA concentration
Drug of choice for myoclonic seizures that may also be used for absence seizures
Valproic acid
Antiepileptic drug that can cause fatal hepatotoxicity and neural tube defects
Valproic acid
Drug of choice for absence seizures
Ethosuximide
Mechanism of action of Ethosuximide
Blocks T-type calcium channels
Antiepileptic drugs that may also be used for bipolar disorder
Valproic acid, carbamazepine, gabapentin
Antiepileptic drug used also for pain of neuropathic origin
Gabapentin
Serious side effect of lamotrigine that makes it require slow titration
Stevens-Johnson Syndrome
Mechanism of action of opioids on analgesia
Activate mu receptors to 1) close presynaptic Ca2+ channels to inhibit neurotransmitter release and 2) open postsynaptic K+ channels to hyperpolarize cell membrane
Side effects of these drugs include nausea and vomiting, euphoria, dependence, sedation, respiratory depression, constipation
Opioids
Tolerance to all effects of opioid agonists can develop except…
Miosis, constipation
Strong opioid agonists
Morphine and fentanyl
Opioid that can be given PO, IV, IM, and intrathecal to relieve anxiety associated with pulmonary edema
Morphine
Opioid available transdermally
Fentanyl
Opioid with antimuscarinic activity
Meperidine
Long-acting opioids used in the management of withdrawal states
Methadone, buprenorphine
Opioid that can cause hyperpyrexic coma with MAOI and serotonin syndrome with SSRI
Meperidine
Moderate opioid agonists
Codeine, hydrocodone, and oxycodone
Partial opioid agonist that has a long duration of action and is resistant to naloxone reversal
Buprenorphine
Opioid antagonist that is given IV
Naloxone
Opioid antagonist that is given orally
Naltrexone
Opioids indicated for use as antitussive
Dextromethorphan, Codeine
Opioids indicated for use as antidiarrheal
Diphenoxylate, Loperamide
Directly proportional to the potency of inhalation anesthetics
Lipid solubility
Inversely proportional to the potency of inhalation anesthetics
Minimal alveolar concentration (MAC)
Inversely proportional to the rate of induction and recovery of inhalation anesthetics
Blood:gas partition coefficient
Mechanism of action of inhalation anesthetics
Potentiation of GABA at GABAa receptors; also reduce Na+ and Ca2+ influx
Currently the only non-halogenated inhalation anesthetic
Nitrous oxide
Inhalation anesthetic with the most analgesic activity
Nitrous oxide
Inhalation anesthetic with the least respiratory and cardiovascular depression and therefore is used frequently as a component of balanced anesthesia
Nitrous oxide
Inhalation anesthetic that can cause fatal hepatotoxicity and cardiac arrhythmia and is no longer used in the US
Halothane
Inhalation anesthetic that is withdrawn from that market due to fatal nephrotoxicity
Methoxyflurane
Inhalation anesthetic that at high concentrations can produce CNS excitation, leading to seizures
Enflurane
Rare, but fatal side effect associated with combination of halogenated inhalation anesthetic and depolarizing blocker
Malingant hyperthermia
Close to ideal inhalation anesthetic that exhibits rapid and smooth induration and recovery, with little organ system toxicity
Sevoflurane
Barbituate used for the induction of anesthesia
Thiopental
A short-acting benzodiazepine commonly used adjunctively with inhalation anesthetics and opioid analgesics for a balanced anesthesia
Midazolam
Opioid safe for use of analgesia and anesthesia during cardiac surgery
Fentanyl
Produces both rapid anesthesia and recovery, has antiemetic activity, but may cause marked hypotension
Propofol
Marked dissociative anesthesia but has significant analgesic activity
Ketamine
Mechanism of action of the intravenous anesthetic that causes dissociative anesthesia
Block NMDA receptor
Side effects of dissociative anesthetic
Cardiovascular stimulation, increased cerebral blood flow, vivid dreams, hallucinations
Neuroleptanesthesia can be produced by a combination of these two agents
Fentanyl and droperidol
Mechanism of action of local anesthetics
Block voltage-gated sodium channels
This condition may necessitate larger doses of local anesthetics because the drugs become ionized and cannot penetrate the neuronal membranes
Low pH
Almost all local anesthetics have this property and sometimes requires the administration of vasoconstrictors to prolong activity
Vasodilation
The only local anesthetic with vasoconstrictive property, but due to abuse potential, only occasionally used for nasal surgery
Cocaine
This type of local anesthetic is more likely to cause hypersensitivity reactions
Ester-type (local anesthetic with one “l” in name)
Local anesthetic most widely used for obstetric anesthesia but causes the most cardiac depression
Bupivacaine
Side effect of most local anesthetics
CNS excitation
Common side 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 delivery to brain
Carbidopa
Two fluctuations in clinical response associated with long-term use of dopamine precursor
“Wearing off” and “on-off phenomenon”
Inhibits monoamine oxidase type B (MAO-B), used as monotherapy for early or mild Parkinson’s disease or adjunct to improve motor function in patients with fluctuations in clinical response
selegiline
Inhibits of catechol-O-methyltransferase (COMT), used as adjunct to improve motor function in Parkinson’s patients with fluctuations in clinical response
Entacapone, tolcapone
Ergot type 2 dopamine receptor (D2) agonist, used for Parkinson’s and restless legs syndrome
Bromocriptine
Non ergot type 2 dopamine receptors (D2) agonist, used for Parkinson’s and restless legs syndrome
Pramipexole and ropinirole
An antiviral that enhances dopamine release for nigrostriatal neurons
Amantadine
A centrally-acting anticholinergic used for tremor and rigidity but have little effect on bradykinesia in patients with Parkinson’s
Benztropine
Drug of choice indicated for familial or essential tremors
Propranolol
Two drugs that inhibit vesicle monoamine transporter used for Huntington’s
Tetrabenazine, reserpine
An antipsychotic with dopamine receptor activity used for Huntington’s
Haloperidol
Three centrally-acting cholinesterase inhibitors used for Alzheimer’s
Donepezil, rivastigmine, galantamine
Noncompetitive antagonist of NMDA receptors used for Alzheimer’s
Memantine
Three main classes of CNS depressant drugs of abuse
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
Mallory-Weiss syndrome, hepatitis, cirrhosis, pancreatitis
Neurological abnormality caused by chronic alcohol abuse and thiamine deficiency
Neurological deficits (Peripheral neuropathy)
Life-threatening alcohol withdrawal syndrome that peaks at 5 days after the last drink
Delirium tremens
Inhibits aldehyde dehydrogenase and used as deterrent for alcohol use
Disulfiram
Opioid receptor antagonist used to prevent alcohol abuse
Naltrexone
Competes for alcohol dehydrogenase and used in methanol or ethylene glycol poisoning
Fomepizole, ethanol
Most commonly abused opioids
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
Opioid
Opioids used for long-term maintenance from opioid withdrawal
Methadone, buprenorphine
Most widely abused sedative hypnotics
Short-acting barbiturates (pentobarbital)
Two date-rape drugs that work through enhancement of GABA receptors in the brain
Flunitrazepam, GHB (gamma-hydroxybutarate)
Benzodiazepine antagonits used to treat benzodiazepine intoxication
Flumazenil
Four major CNS stimulant drugs of abuse
Caffeine, nicotine, cocaine, amphetamines
Treatments available for nicotine addiction
Patch, gum, lozenge, buproprion, 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
Methamphetamine (crystal meth), MDMA (methylenedioxymethamphetamine, 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, or angel dust)
Synthetic ergot derivative that can produce perceptual hallucinations and used as an illicit drug; pay cause paranoia
LSD (lysergic acid diethylamide)
Active ingredietni s tetrahydrocannabinol (THC); side 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
Antipsychotics that repress primarily the positive symptoms of schizophrenia
Typical antipsychotics
Primary mechanism of action of typical antipsychotics
Inhibits D2 receptors
Common endocrine side effects of all typical antipsychotic drugs
Hyperprolactinemia, galactorrhea
Two low potency, typical antipsychotic drugs
Chlorpromazine, thioridazine
Typical antipsychotic associated with retinopathy and cardiac toxicity
Thioridazine
Common side effects of low potency typical antipsychotic drugs
Dry mouth (anticholinergic), sedation (antihistamine), hypotension (alpha1 block)
Three high potency, typical antipsychotic drugs
Haloperidol, fluphenazine, trifluoperazine
Typical antipsychotic that can also be used for Tourette syndrome
Haloperidol
Side effects more commonly associated with high potency typical antipsychotic drugs
Dystonia, akathisia, bradykinesia, tardive dyskinesia (extrapyramidal symptoms)
Life-threatening side 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
Two atypical antipsychotics that can cause weight gain
Clozapine, olanzapine
Two atypical antipsychotics that can prolong the QT interval
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 syndrome
Aripiprazole
Tricyclic antidepressants
-iptuline, -ipramine, dozepine, amoxapine
Mechanism of tricyclic antidepressants
Block serotonin and norepinephrine reuptake
Common side effects of tricyclic antidepressants
Autonomic (block muscarinic and alpha1), sedation
Tricyclic secondary amines that produce less sedation and autonomic side effects (compared with tricyclic tertiary amines)
Nortriptyline, desipramine
Three life-threatening side effects associated with tricyclic antidepressants
Convulsion, cardiotoxicity, coma (3 C’s)
Tricyclic antidepressent 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 side 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)
Four selective serotonin reuptake inhibitors
Fluoxetine, paroxetine, sertraline, citalopram
Serious side effect of SSRIs when used with other drugs such as MAOIs, SNRIs, or TCAs
Serotonin syndrome
Two selective serotonin-norepinephrine reuptake inhibitors (SNRIs)
Duloxetine, venlafaxine
Class of drug 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
Buproprion
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
Side effects of lithium
Tremor, hypothyroidism, nephrogenic diabetes insipidus, fetal cardiac defects
Antineoplastic folic acid analogue that inhibits dihydrofolate reductase
Methotrexate
Antineoplastic pyrimidine analog that inhibits thymidylate synthetase
5-flurouracil (5-FU)
Antineoplastic pyrimidine analog that inhibits DNA polymerase
Cytarabine
Serious side effect associated with cytarabine
Pancytopenia
Three antineoplastic purine analogs that inhibit purine synthesis
Azathioprine, 6-mercaptopurine, 6-thioguanine
Drug used concurrently with antineoplastics to reduce renal precipitation of urates
Allopurinol
Two antineoplastics that require dose-reduction in patients who are taking allopurinol
Azathioprine, 6-mercaptopurine
Inhibits microtubule formation by binding to beta-tubulin; dose-limiting side effect is bone marrow suppression
Vinblastine
Inhibits microtubule formation by binding to beta-tubulin; dose-limiting side effect is neurotoxicty
Paclitaxel, -taxels
Two prodrugs, that after liver bioactivation, bind to N7 nitrogen of guanine and cross-link DNA
Cyclophosphamide, ifosfamide
Serious side effect of cyclophosphamide and ifosfamide due to generation of acrolein
Hemorrhagic cystitis
Agents that is used to bind acrolein and prevent drug-induced hemorrhagic cystitis
Mesna
Nitrosureas that spontaneously form active intermediates that cross-link DNA; can cross blood-brain-barrier and is indicated for brain tumors
Carmustine, -mustines
Alkylating agent that has greater activity against myeloid cells than lymphoid cells; serious side effects include myelosuppression and pulmonary fibrosis
Busulfan
Two anthracyclines that chelate DNA, form free radicals, and cause dose-limiting cardiotoxicity
Daunorubicin, doxorubicin
