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199 Cards in this Set
- Front
- Back
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3 zones of adrenal cortex and their products
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Glomerulosa (mineralcorticoids), fasiculata (glucocorticoids = GC), and reticularis (adrenal androgens)
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Mnemonic for 3 zones of adrenal cortex
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GFR
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Used for Addison's disease, Congenital Adrenal Hyperplasia (CAH), inflammation, allergies, and asthma (as local inhalation)
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Glucocorticoids
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Short-acting glucocorticoids
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Cortisone & hydrocortisone (equivalent to cortisol)
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Intermediate-acting glucocorticoids
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Prednisone, methylprednisolone, prednisolone, and triamcinolone
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Long-acting glucocorticoids
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Betamethasone and dexamethasone
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Mineralocorticoids
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Fludrocortisone and deoxycorticosterone
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Some side effects of corticosteroids *
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Osteopenia, impaired wound-healing, incr risk of infx, incr appetite, HTN, edema, PUD, euphoria, psychosis, stria, thinning of the skin
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Period of time after which GC therapy would need to be tapered to be discontinued
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5-7 days
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Test used for Cushing's syndrome (increased corticosteroid)
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Dexamethasone suppression test
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Inhibits conversion of cholesterol to pregnenolone therefore inhibiting corticosteroid synthesis
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Aminoglutethimide
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Antifungal agent used for inhibition of all gonadal and adrenal steroids
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Ketoconazole
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Antiprogestin used as potent antagonist of GC receptor
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Mifepristone
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Diuretic used to antagonize aldosterone receptors *
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Spironolactone
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Common SE of spironolactone **
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Gynecomastia and hyperkalemia
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Disease caused by excess ergot alkaloids
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St. Anthony's Fire (Ergotism)
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Term for endogenous substances commonly interpreted as histamine, serotonin, prostaglandins, and vasoactive peptides
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Autocoids
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Syndrome of hypersecretion of gastric acid and pepsin usually caused by gastrinoma; it is usually associated with severe gastric ulceration and diarrhea
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Zollinger-Ellison Syndrome
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Drug/autocoid that causes contraction of the uterus *
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Oxytocin
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Distribution of histamine receptors: H1, H2, and H3 *
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H1: Smooth muscle; H2: Stomach, heart, mast cells; H3: CNS, nerve endings
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Prototype antagonist of H1 receptors and H2 receptors *
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H1: Diphenhydramine; H2: cimetidine
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1st generation antihistamine that is highly sedating **
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Diphendydramine
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1st generation antihistamine that is least sedating
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Chlorpheniramine or cyclizine
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2nd generation antihistamines *
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Fexofenadine, loratadine, cetirizine
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Generation of antihistamine that has the most CNS effects
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First generation due to being more lipid- soluble
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Major indication for use of H1 receptor antagonist
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Use in IgE mediated allergic reaction
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Antihistamine that can be used for anxiety & insomnia and is not addictive
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Hydroxyzine (Atarax)
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H1 antagonist used in motion sickness
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Dimenhydrinate, meclizine, and other 1st gens
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Most common side effect of 1st generation antihistamines
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Sedation
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Lethal arrhythmias resulting from concurrent therapy with azole fungals (metabolized by CYP 3A4) and these antihistamines, which inhibit the 3A4 iso-enzyme.
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Terfenadine and astemizole (have been removed from the market)
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H2 blocker that causes the most interactions with other drugs *
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Cimetidine
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Clinical use for H2 blockers
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Acid reflux disease, duodenal ulcer and peptic ulcer disease
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5-HT 1d receptors (for serotonin) are located
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Mostly in the brain, and they mediate synaptic inhibition via incr K+ conductance
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5-HT 2 receptors are located
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Smooth muscle, platelets
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5-HT 3 receptors are located
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Area postrema (CNS), sensory and enteric nerves
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5-HT 1d agonist used for migraine headaches **
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Sumatriptan, naratriptan, and rizatriptan
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Triptan available in parenteral and nasal formulation
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Sumatriptan
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H1 blocker that is also a serotonin antagonist
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Cyproheptadine
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Agents for reduction of postpartum bleeding **
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Oxytocin, ergonovine and ergotamine
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Agents used in treatment of carcinoid tumor **
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Ketanserin (not avail in USA), cyproheptadine, and phenoxybenzamine
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5-HT 3 antagonist used in chemotherapy induced emesis ***
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Ondansetron, granisetron, dolasetron, and alosetron
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5-HT 3 antagonist that has been associated with QRS and QTc prolongation and should not be used in patients with heart disease
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Dolasetron
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DOC to treat chemo-induced nausea and vomiting **
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Odansetron
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Drug used in ergot alkaloid overdose, ischemia, and gangrene
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Nitroprusside
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Reason ergot alkaloids are contraindicated in pregnancy
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Uterine contractions
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SE of ergot alkaloids
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Hallucinations resembling psychosis
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Ergot alkaloid used as an illicit drug *
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LSD
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Dopamine agonist used in hyperprolactinemia *
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Bromocriptine
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Common side effect of hypnotic agents
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Sedation
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Occurs when sedative hypnotics are used chronically or at high doses
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Tolerance
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The most common type of drug interaction of sedative hypnotics with other depressant medications
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Additive CNS depression
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Benzodiazepines used to promote sleep
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Temazpam, trizolam, flurazepam
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Benzodiazepine used for anxiety
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Alprazolam
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Non-benzodiazepine used as an anxiolytic
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Buspirone
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Non-benzodiazepine used for sleep
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Zolpidem
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Major effect of benzodiazepines on sleep at high doses *
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REM is decreased
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Neurologic SE of benzodiazepines
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Anterograde amnesia
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Reason benzos are used cautiously in pregnancy *
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Ability to cross the placenta
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Main route of metabolism for benzodiazepines
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Hepatic
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Benzodiazepines that undergo extrahepatic conjugation (useful in older or hepatically impaired pts.)
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Lorazepam, oxazepam, temazepam
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MOA for benzodiazepines
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Increase the FREQUENCY of GABA- mediated chloride ion channel opening
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Antidote to benzodiazepine overdose (antagonist that reverses the CNS effects) *
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Flumazenil
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Benzodiazepine with useful relaxant effects in skeletal muscle spacicity of central origin
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Diazepam
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Benzodiazepine that has efficacy against absence seizures and in anxiety states (e.g. Agoraphobia)
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Clonazepam
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Benzodiazepines that are the most effective in the treatment of panic disorder
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Alprazolam and Clonazepam
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Benzodiazepine that is used for anesthesia
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Midazolam
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DOC for status epilepticus
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Diazepam
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Longer acting benzodiazepines used in the management of withdrawal states of alcohol and other drugs
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Chlordiazepoxide and diazepam
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Agents having active metabolites, long half lives, and a high incidence of adverse effects
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Diazepam, Flurazepam, chlordiazepoxide, and clorazepate
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Barbiturates may precipitate this hematologic condition
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Acute intermittent porphyria
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Barbiturates decrease the effectiveness of many other drugs via this pharmacokinetics property
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Liver enzyme INDUCTION
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Barbiturates MOA
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Incr DURATION of GABA-mediate chloride channels
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Barbiturate used for the induction of anesthesia
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Thiopental
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Site of action for zaleplon and zolpidem
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Benzodiazepine receptor BZ1 (although do not have benzodiazepine ring structure)
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Good hypnotic activity with less CNS SE than most benzodiazepines
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Zolpidem, zaleplon
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Agent that is a partial agonist for the 5-HT 1A receptor
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Buspirone
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Drug of choice for generalized anxiety disorder, NOT effective in acute anxiety
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Buspirone
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Most frequent route of metabolism
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Hepatic enzymes
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Mechanisms of action for Phenytoin, Carbamazepine, Lamotrigine
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Sodium channel blockade
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MOA for benzodiazepines and barbiturates
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GABA-related targets
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MOA for Ethosuximide
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Calcium channels
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MOA for Valproic acid at high doses
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Affect calcium, potassium, and sodium channels
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Drugs of choice for generalized tonic-clonic and partial seizures *
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Valproic acid and Phenytoin
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DOC for febrile seizures
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Phenobarbita
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Drugs of choice for absence seizures *
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Ethosuximide and valproic acid
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Drug of choice for myoclonic seizures *
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Valproic acid
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Drugs of choice for status epilepticus
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IV diazepam for short term (acute) treatment; phenytoin for prolonged therapy
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Drugs that can be used for infantile spasms
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Corticosteroids
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Antiseizure drugs also used for Bipolar Affective Disorder (BAD)
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Carbamazepine, valproic acid, phenytoin, and gabapentin
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Anti-seizure drugs used also for Trigeminal neuralgia
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Carbamazepine
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Anti-seizure drugs used also for pain of neuropathic orgin *
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Gabapentin
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Anti-seizure agent that exhibits non-linear metabolism, highly protein bound, causes fetal hydantoin syndrome, and stimulates hepatic metabolism
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Phenytoin
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SE of phenytoin *
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Gingival hyperplasia, nystagmus, diplopia and ataxia
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Anti-seizure agent that induces formation of liver drug-metabolism enzymes, is a teratogen and can cause craniofacial anomalies and spina bifida
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Carbamazepine
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Agent that inhibits hepatic metabolism, is hepatotoxic and teratogen that can cause neural tube defects and gastrointestinal distress
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Valproic acid
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Laboratory values required to be monitored for patients on valproic acid
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Serum ammonia and LFT's
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SE for Lamotrigine
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Stevens-Johnson syndrome
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SE for Felbamate
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Aplastic anemia, acute hepatic failure
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Anti-seizure medication also used in the prevention of migraines
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Valproic acid
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Carbamazepine may cause
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Agranulocytosis
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Anti-seizure drugs used as alternative drugs for mood stabilization
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Carbamazepine, gabapentin, lamotrigine, and valproic acid
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Agent used in drug therapy of Parkinson's instead of Dopamine which has low bioavailability and does not cross the BBB
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L-dopa
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This is combined with L-dopa, inhibits DOPA decarboxylase (active only peripherally) which allows lower effective doses of L-dopa and allows for fewer SE's (GI distress, postural hypotension, and dyskinesias)
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Carbidopa
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Clinical response that may fluctuate in tx of Parkinson's dx
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"On-off phenomenon"
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Anti-Parkinson's drug which increases intraocular pressure and is contraindicated in closed angle glaucoma
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Levodopa
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Ergot alkaloid that is a partial agonist at D2 receptors in the brain, used for patients who are refractory or cannot tolerate levodopa, causes erythromelalgia
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Bromocriptine
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Non ergot agents used as first-line therapy in the initial management of Parkinson's
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Pramipexole and ropinirole
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Enhances dopaminergic neurotransmission, SE's include CNS excitation, acute toxic psychosis and livedo reticularis
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Amantadine
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Inhibitor of MAO type B which slows down metabolism of dopamine, used adjunct to levodopa or as sole agent in newly diagnosed patients
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Selegiline
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Inhibitors of catechol-O-methyltransferase (COMT), used as adjuncts in Parkinson's dx and cause acute hepatic failure (monitor LFT's)
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Tolcapone
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Agent decreases the excitatory actions of cholinergic neurons. May improve tremor and rigidity but have LITTLE effect on bradykinesia. Atropine-like side effects
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Benztropine
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Agent effective in physiologic and essential tremor
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Propranolol
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Agents used in Huntington's Disease
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Tetrabenazine (amine depleting drug), reserpine
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Agents used in Tourette's Disease
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Haloperidol, pimozide , clonidine
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Chelating agent used in Wilson's Disease
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Penicillamine
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Irreversible condition resulting from the use of antipsychotics, reserpine at high doses, and MPTP (by-product of illicit meperidine analog) *
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Drug induced Parkinsonism
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Example of three antidepressants that are indicated for obsessive compulsive disorder
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Clomipramine, fluoxetine and fluvoxamine
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Neurotransmitters affected by the action of antidepressants
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Norepinephrine and serotonin
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Usual time needed for full effect of antidepressant therapy
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2 to 3 weeks
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Population group especially sensitive to side effects of antidepressants
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Elderly patients
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All antidepressants have roughly the same efficacy in treating depression, agents are chosen based on these criterion
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Side-effect profile and prior pt response
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Well-tolerated and are first-line antidepressants
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SSRI's, bupropion, and venlafaxine
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Most useful in patients with significant anxiety, phobic features, hypochondriasis, and resistant depression
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Monamine oxidase inhibitors
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Condition will result from in combination of MAOI with tyramine containing foods (ex. wine, cheese, and pickled meats)
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Hypertensive crisis
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MAOI should not be administered with SSRI's or potent TCA's due to development of this condition
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Serotonin syndrome
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Sedation is a common side effect of these drugs, they lower seizure threshold; uses include BAD, acute panic attacks, phobias, enuresis, and chronic pain; overdose can be deadly
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Tricyclic Antidepressants (TCAs)
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Three C's associated with TCA toxicity
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Coma, Convulsions, Cardiac problems (arrhythmias and wide QRS)
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Agents having higher sedation and antimuscarinic effects than other TCA's
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Tertiary amines (less polar than quaternary amines)
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TCA used in chronic pain, is a hypnotic, and has marked antimuscarinic effects
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Amitriptyline
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TCA used in chronic pain, enuresis, and ADD *
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Imipramine
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TCA with greatest sedation of this group, and marked antimuscarinic effects, used for sleep
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Doxepin
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TCA used in obsessive compulsive disorder (OCD), most significant of TCA's for risk of seizure, weight gain, and neuropsychiatric signs and symptoms
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Clomipramine
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Secondary amines that have less sedation and more excitation effect
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Nortriptyline, Desipramine
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Side effects seen with tricyclic antidepressants
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Muscarinic blockade (dry mouth, constipation); weak alpha-1 block (orthostatic hypotension); weak hisamine block (sedation)
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Antidepressant associated with neuroleptic malignant syndrome
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Amoxapine
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Antidepressant associated with seizures and cardiotoxicity
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Maprotiline
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Antidepressant having stimulant effects similar to SSRI's and can increase blood pressure
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Venlafaxine
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Antidepressant inhibiting norepinephrine, serotonin, and dopamine reuptake
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Venlafaxine
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Antidepressant also used for sleep that causes priapism
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Trazodone
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Antidepressant which is inhibitor of CYP450 enzymes and may be associated with hepatic failure
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Nefazodone
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Heterocyclic antidepressants least likely to affect sexual performance, used for management of nicotine withdrawal; SE's include dizziness, dry mouth, aggravation of psychosis, and seizures *
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Bupropion
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Antidepressant with MOA as alpha 2 antagonist, has effects on both 5-HT and NE, blocks histamine receptors, and is sedating
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Mirtazapine
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SE of mirtazapine
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Liver toxicity, increased serum cholesterol
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Except for these agents all SSRI have significant inhibition of CYP450 enzymes
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Citalopram and its metabolite escitalopram
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Side effects frequently seen with SSRIs
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CNS stimulation, GI upset
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Antidepressants with no effect on BP, no sedation
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SSRIs
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SSRI with long T1/2 and can be administered once weekly for maintenance, not for acute tx
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Fluoxetine
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SSRI indicated for premenstrual dysphoric disorder
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Fluoxetine (Sarafem)
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Some of SSRIs' therapeutic effects beside depression
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Panic attacks, social phobias, bulimia nervosa, and PMDD (premenstrual dysphoric disorder), OCD
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SSRI less likely to cause a withdrawal syndrome
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Fluoxetine
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This agent has greater affinity for muscarinic receptors and used for postoperative and neurogenic ileus and urinary retention *
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Bethanechol
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Only direct acting agent that is very lipid soluble and used in glaucoma
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Pilocarpine
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This agent used to treat dry mouth in Sjögren's syndrome
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Cevimeline
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Indirect-Acting ACh Agonist, alcohol, short DOA and used in diagnosis of myasthenia gravis
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Edrophonium
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Carbamate with intermediate action, used for+A1170 postoperative and neurogenic ileus and urinary retention
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Neostigmine
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Treatment of atropine overdose and glaucoma (because lipid soluable). Enters the CNS rapidly and has a stimulant effect, which may lead to convulsions
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Physostigmine
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Treatment of myasthenia gravis
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Pyridostigmine
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Antiglaucoma organophosphate
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Echothiophate
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Associated with an increased incidence of cataracts in patients treated for glaucoma
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Long acting cholinesterase inhibitors
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Scabicide organophosphate
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Malathion
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Organophosphate anthelmintic agent with long DOA
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Metrifonate
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Toxicity of organophosphates (mnemonic): *
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DUMBELSS (diarrhea, urination, miosis, bronchoconstriction, excitation of skeletal muscle and CNS, lacrimation, salivation, and sweating)
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The most frequent cause of acute deaths in cholinesterase inhibitor toxicity
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Respiratory failure
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The most toxic organophosphate
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Parathion
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Treatment of choice for organophosphate overdose
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Atropine
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This agent regenerates active cholinesterase and is a chemical antagonist used to treat organophosphate exposure
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Pralidoxime
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Prototypical drug is atropine
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Nonselective muscarinic antagonists
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Treat manifestations of Parkinson's disease and EPS (extrapyramidal symptoms) *
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Benztropine, trihexyphenidyl
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Treatment of motion sickness *
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Scopolamine, meclizine
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Produce mydriasis and cycloplegia *
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Atropine, homatropine, C1208 tropicamide
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Bronchodilation in asthma & COPD *
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Ipratropium
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Reduce transient hyper GI motility
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Dicyclomine, methscopolamine
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Cystitis, postoperative bladder spasms, or incontinence
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Oxybutynin, dicyclomine
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Toxicity of anticholinergics
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Block SLUD (salivation, lacrimation, urination, defecation)
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Another mnemonic for anticholinergic toxicity
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"Dry as a bone, red as a beet, mad as a hatter, hot as a hare, blind as a bat"
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Atropine fever is the most dangerous effect and can be lethal in this population group
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Infants
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Contraindications to use of atropine
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Infants, closed angle glaucoma, prostatic hypertrophy
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The limiting adverse effect of ganglion blockade that patients usually are unable to tolerate
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Severe HTN
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Reveral of blockade by neuromuscular blockers
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Cholinesterase inhibitors
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Tubocurarine is the prototype of this group; pancuronium, atracurium, vecuronium are newer short acting agents; produce competitive block at end plate nicotinic receptor, causing flaccid paralysis
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Nondepolarizing Neuromuscular Blockers
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Only member of depolarizing neuromuscular blocker group; causes fasciculation during induction and muscle pain after use; has short duration of action
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Succinylcholine
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Chemical antagonists that bind to the inhibitor of Ach-Estrase and displace the enzyme (if aging has not occurred)
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Pralidoxime (Cholinesterase regenerator)
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Used to treat patients exposed to insecticides such as parathion
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Pralidoxime and atropine
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MOA of penicillin
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Block cell wall synthesis by inhibiting peptidoglycan cross-linkage
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Drug used for MRSA *
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Vancomycin
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Vancomycin MOA **
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Blocks cell wall synthesis by sequestration
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Genetic basis of low level resistance found with vancomycin
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Point mutation
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Penicillins active against penicillinase secreting bacteria
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Methicillin, nafcillin, and dicloxacillin
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Cheap wide spectrum antibiotic DOC for otitis media ***
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Amoxicillin
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Class of antibiotics that have 10% cross sensitivity with penicillins
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Cephalosporins
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PCN active against pseudomonas
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ceftazidime, imipenem, piperacillin and ticarcillin
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Antibiotic causing red-man syndrome, and prevention
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Vancomycin, infusion
at a slow rate and antihistamines |
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Treatment of resistant pseudomembranous colitis
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ORAL vancomycin
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Cephalosporins able to cross the BBB
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Cefuroxime (2nd) generation, Ceftazidime, Ceftriaxone, Cefotaxime
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Oral 3rd generation cephalosporins NOT able to cross the BBB
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Cefixime
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Drug used for N. gonorrhea in females *
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Ceftriaxone
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Cephalosporin causes kernicterus in neonates
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Ceftriaxone or cefuroxime
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Lactam that can be used in PCN allergic patients
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Aztreonam/carbapenems
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SE of imipenem
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Seizures
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