Lange - Pharm Flashcards

Question

Nucleotide Reverse Transcriptase Inhibitors (-fovirs): Tenofovir, Adefovir

Answer 1

* Don't need phosphorylated * inhibit reverse transcriptase * Uses = **HIV and Hepatitis B** infections

Answer 2

* Bind specifically to reverse transcriptase--\>decreased DNA synthesis * Use = HIV HAART therapy * SE:**Nevirapine**--\>Stevens-Johnson syndrome; fulminant hepatitis, **induce p-450 system** * **Efavirenz**--\>delusion and nightmares (CNS disturbances) * **Delavirdine**--\> teratogenic, elevated LFTs

Answer 3

* inhibit HIV protease--\>no mature proteins cleaved--\>virus is unable to replicate * Uses = HIV HAART therapy * SE = altered body fat distribution (Cushingoid)/hyperlipidemia * **Ritonavir** - **inhibit P-450**--\> increase serum levels of other durgs

Answer 4

* Viral thymidine kinase--\>phosphorylates (activates) acyclovir--\>dGTP analogue--\>incorporates--\>inhibits viral DNA synthesis * Uses = HSV1, HSV2, VZV, EBV (oral hairy leukoplakia)--Herpes mostly! * **SE = nephrotoxicity (via crystallization); neurotoxicity (delirium, tremor)**

Answer 5

* Viral kinase--\>phosphorylates (activates) ganciclovir--\>guanosine analogue--\>inhibits CMV DNA polymerase--\>decreased CMV DNA synthesis * Uses = CMV infections, especially CMV retinitis * SE = pancytopenia

Answer 6

* Pyrophosphate analogue--\>inhibits viral DNA polymerase * But does not require kinase activation! * Use = 2DOC for CMV infections and acyclovir-resistant HSV/VZV infections * SE = nephrotoxicity (--\>hypoCa and hypoMg--\>szs)

Answer 7

* Binds M2--\>blocks uncoating of viral RNA * Use = reduce length of influenza A symptoms * Also stimulates DA release from SN (Can help tx Parkinson's) * SE = CNS sx

Answer 8

* Inhibits Neuraminidase--\>decreased viral replication/release * Use = tx and prophylaxis of both influenza A and B

Answer 9

* Guanosine analogue--\>inhibits viral 'R'NA polymerase--\>inhibits viral 'r'eplication * Uses = 'R'SV bronchiolitis

Answer 10

* Binds ergosterol--\>pores (altered cell membrane permeability)--\>cell death * Uses = systemic mycotic infections * SE = nephrotoxic (--\>hypoK and hypoMg) * Can--\>arrhythmias * Can't cross BBB, so give intrathecally for fungal meningitis

Answer 11

* Similar MOA to Amphotocerin B * More toxic so only used topically for oral and cutaneous Candida

Answer 12

* "FlU = 5FU" * Converted into 5-FU (nucleotide analogue) inside fungal cell--\>inhibits thymidylate synthase--\>inhibits fungal DNA and RNA synth * Use = added to amphotocerin B to combat fungal meningitis and systemic fungal infections

Answer 13

* **Inhibits glucan synthase**--\>disrupts polysaccharide fungal cell wall * Tx of systemic fungal infections

Answer 14

* Inhibits fungal P450--\>inhibits ergosterol synthesis * Also inhibits our P450--\>disrupted gonadal and adrenal steroid synth--\>gynecomastia, decreased libido, etc * Uses = broad-spectrum antifungal * Can be given as an antifungal vaginal suppository (for vaginal candidiasis) * Also used to tx Cushing syndrome

Answer 15

* Same as ketoconazole (inhibits P450) * But doesn't affect mammal steroid synth as much! Means no gynecomastia * Uses = systemic fungal infections * Especially cryptococcal meningitis (Lifelong prophylaxis) and Candidal sepsis

Answer 16

* Interferes with microtubule function in keratin-rich tissues--\>inhibits mitosis--\>inhibits fungal cell replication * Uses = oral antifungal for dermatophytic fungal infections (like tinea corporis)

Answer 17

* Also for dermatophytic fungal infections * Inhibits squalene epoxidase--\>decreased ergosterol synthesis

Answer 18

* Tx of Plasmodium falciparum and blood form of the others * Quinine and mefloquine tx Plasmodium falciparum if it is drug resistant * Quinine SE = Cinchonism (tinnitus, H/A, dizziness)

Answer 19

* Inhibits DHFR--\>decreased DNA synthesis * (Like Tri"meth"oprime) * Uses = tx and prophylaxis of Plasmodium falciparum and tx of **Toxoplasma gondii**

Answer 20

* Uses = tx hepatic forms of P. vivax and P. ovale * Don't give in pregnancy (--\>fetal hemolytic anemia)

Answer 21

* Prophylaxis for PCP (like Dapsone)

Answer 22

Tx of Trypanosoma cruzi (Chagas)

Answer 23

* Tx of early Trypanosoma brucei infections * (=African sleeping sickness with recurring fever and LAD...tsetse fly)

Answer 24

* Tx of late Trypanosoma brucei infections * (It "sure" is nice to go to sleep. And melatonin helps with sleep.)

Answer 25

* Tx of Leishmaniasis * (=spiking fevers, HSM...sandfly)

Answer 26

* B agonist at low doses, alpha agonist as well at high doses. * Note: so at low doses it decreases DBP, at high doses it increases DBP (SBP gets increased no matter what) * Low doses--\>increased HR and contractility, bronchodilation * High doses--\>vasoconstriction too * Uses = anaphylaxis, cardiac arrest, severe hypotension, bronchospasm in asthma, wide angle glaucoma (increased ciliary body aqueous humor)

Answer 27

* Potent alpha1, alpha2, and beta1 agonist * alpha1--\>vasoconstriction * beta1--\>increased contractility and HR (but get reflex bradycardia--\>HR doesn't change) * Uses = tx of severe hypotension and shock

Answer 28

* Low doses = beta1/2 and D1 agonist--\>increased HR, contractility * D1--\>increases renal and splanchnic blood flow--\>promotes renal perfusion * High doses = alpha 1 agonist--\>vasoconstriction * Uses = pressor in emergency tx of severe hypotension and shock, but spares kidneys!!!

Answer 29

* B1 agonist--\>increases HR and contractility * Uses = tx of cardiogenic shock * Increases myocardial O2 consumption

Answer 30

* Stimulates release of NE and epi from neurons--\>increased SBP and DBP and bronchodilation * Also stimulates CNS--\>insomnia and decreased appetite * Uses = nasal decongestant, wt loss, athletic enhancement

Answer 31

* Blocks NA/K ATPase that is responsible for reuptake of NE, DA, and 5-HT. Block voltage-gated Na+ channels. * --\>euphoria (d/t DA), vasoconstriction, and cardiac ischemia * SE = HTN, cardiac ischemia, cardiac arrhythmias, abuse

Answer 32

* A1 agonist--\>vasoconstriction and pupil dilation; Nasal constriction if applied topically * Uses = severe hypotension and shock, dilate pupils for ophtho exam, nasal congestion (but get rebound rhinorrhea after a few days)

Answer 33

* A2 agonist--\>decreased central adrenergic activity--\>decreased vasoconstriction, decreased CO and decreased HR * Does not decrease renal blood flow (good for HTN pts with renal dz) * Uses = tx of HTN * SE = rebound HTN (if drug is withdrawn quickly)

Answer 34

* Potent B1 and B2 agonist--\>increased HR/contractility, vasodilation (d/t B2), and bronchodilation * Uses = tx of torsades de pointes, or sometimes cardiac arrest or complete heart block

Answer 35

* Short-acting B2 agonist--\>bronchodilation * B2 can also--\>**K shifting** into cell * Use = asthma, including DOC for acute episodes * Also can be used to tx hyperkalemia at high doses

Answer 36

* Similar to Ephedrine. * --\>hyperaroused state. * Also decreased appetite and insomnia.

Answer 37

* Amphetamine derivative. * Uses = narcolepsy, ADHD * But Modafinil is DOC for narcolepsy I think

Answer 38

* Reserpine: * Inhibits neuron's ability to store NE, DA, and 5-HT * --\>depletion of these NTs * Uses = tx of HTN, but causes serious psych depression so not used much! * Guanethidine--similar, for HTN, but also not used much anymore

Answer 39

* "Middledrine" * A1 agonist--\>vasoconstriction * Use = orthostatic hypotension * SE = supine HTN

Answer 40

* A2 agonist--\>decreased central adrenergic activity--\>decreased vasoconstriction * Also does not reduce renal blood flow * Use = tx of moderate HTN * SE = orthostatic HTN, dizziness * Very similar to Clonidine!

Answer 41

* D1 agonist--\>splanchnic/renal vasodilation and natriuresis * **= only available agent that improves renal perfusion while lowering bp!** * Use = **HTN emergencies**

Answer 42

Similar to Albuterol, but long-acting, so used to prevent asthma and COPD attacks

Answer 43

* B2 agonist--\>relaxes uterus and bronchodilates * Uses = only use if preterm labor needs to be delayed greater than 48 hours (like if CS need to be given for fetal lung maturity) * SE = tachycardia, tremor

Answer 44

B2 agonist--\>reduced preterm labor uterus contractions

Answer 45

* Irreversible alpha receptor antagonist (a1\>a2)--\>decreased vasoconstriction--\>decreased bp * Use = **tx of pheochromocytoma** (or given before surg on pheochromocytoma)

Answer 46

* Reversible alpha receptor antagonist. * Use = to **dx pheochromocytomas** * (Pt will get a larger than expected bp decrease)

Answer 47

* Selective alpha1 antagonist--\>decreased vasoconstriction and decreased bladder/prostate contraction (relax internal urethral spincter) * Uses = HTN + BPH * SE = "first-dose" syncope (so start with low dose)

Answer 48

* B1 and B2 antagonist--\>decreased HR/contractility and bronchoconstriction * Uses = tachycardia with hyperthyroidism, HTN/CAD, chronic migraine tx * SE = bronchoconstriction, fasting hypoglycemia, hyperkalemia (bc interfere with B2-mediated IC K uptake) * Hypoglycemia bc decrease NE/epi release in response to glucose * So don't use in DM pts (mask hypoglycemia sx!)

Answer 49

* "Tim-e 2 fix these eyes" * B1 and B2 antagonist. * B2 block--\>decreased aqueous humor production by ciliary epithelium--\> tx of wide-angle glaucoma

Answer 50

* A1 and B1/2 receptor blocker--\>lower bp, lower HR/contractility, bronchoconstriction * --\>decreased cardiac work * Uses = chronic CHF; HTN

Answer 51

* B1 receptor antagonist--\>decreased HR/contractility/conductance (increased PR)--\>decreased CO * (also get a little bronchoconstriction d/t mild B2 antagonism) * Remember: B1 also is on renal JG cells, so this decreases renin * Uses = HTN, CAD, tachycardias * Esmolol = short-acting, for critically ill pts

Answer 52

* Competitive inhibition of Nicotinic receptors on the postsynaptic neuron of the autonomic ganglia. * Tx HTN emergencies * SE: hypotension

Answer 53

* M1-M2-M3 (mostly M3) agonist--\>pupillary sphincter muscle contraction and ciliary muscle contraction * "P"upillary sphincter muscle contraction--\>open canal of Schlemm--\>anterior chamber gets wider--\>tx of narrow angle glaucoma * "C"iliary muscle contraction--\>open trabecular meshwork--\>tx of wide angle glaucoma * Uses = tx of both narrow angle and wide angle glaucoma

Answer 54

Also used to tx wide-angle glaucoma (like Pilocarpine)

Answer 55

* Inhaled M1-M2-M3 (mostly "M"3) agonist--\>smooth muscle contraction of bronchi * Use = bronchial challenge test for dx of reactive airway disease

Answer 56

* M2-M3 (mostly M3) agonist--\>increases "b"ladder contraction and relaxes bladder sphincter--\>promotes urination * Use = tx urinary retention (example: atonic bladder after surg) * Also used to tx neurogenic ileus * SE = bradycardia/HTN (d/t M2), diarrhea, sweating (d/t M3)

Answer 57

* Competitive M1-M2-M3 antagonist * Block M1--\>psychosis * Block M2--\>tachycardia * Block M3--\>cycloplegia (loss of accommodation d/t paralyzed ciliary muscle), mydriasis, decreased GI motility * Use = tx for bradycardia during cardiac emergencies; and antidote for AChE inhibitor\* poisoning (nerve gas, insecticide) * SE = hyperthermia, flushing, decreased salivation...tachycardia

Answer 58

* Antidote for Atropine overdose * Used bc it can cross the BBB

Answer 59

* Competitive M1-M2-M3 antagonist--\>crosses BBB and blocks M1--\>interferes with neuronal communication b/w vestibular ear and CTZ--\>prevents motion sickness * Use = tx for motion sickness * Also can help muscarinic sx d/t stigmines (which tx MG) * SE = "ABCCDSS" (cholinergic blockade)

Answer 60

* "Check your eyes: The Benz is getting balanced on Park place" * M1-M2-M3 antagonist--\>crosses BBB and acts on M1 in SN--\>decreased cholinergic activity (Ach)--\>restore DA-Ach balance--\>helps Parkinson's * DOC for drug-induced PD * Use = adjuvant for PD, improves the tremor and rigidity (but not the bradykinesia) * C/I in pts with narrow angle glaucoma (d/t M3 inhibition) * --\>pupil spincter muscle relaxes and blocks Canal of Schlemm * Other anti-PD agents = DA agonists (Bromocriptine, Amantadine, Levodopa) and MAO-B inhibitors (Selegiline)

Answer 61

* M3 antagonist--\>bronchodilation * Use = tx of COPD and asthma * Especially in pts who cannot take adrenergic agents

Answer 62

* "If you're nine you pee your pants so you need Oxybut-nine" * M1-M2-M3 antagonist--\>constricts bladder spincter and decreases bladder contraction * Use = tx of urinary incontinence * SE = cholinergic blockage * Propantheline: same action. Urinary incontinence and duodenal ulcers

Answer 63

* Neo--3 letters = 3 uses * **Reversibly inhibits AChE-**-\>increased stimulation of both nicotinic and muscarinic receptors * Uses = tx of myasthenia gravis * Also, to stimulate the GI tract and bladder postoperatively * Also, to overcome non-depolarizing NM blockade

Answer 64

* Similar, but crosses BBB. * \*Uses = tx of atropine poisoning * Also tx of glaucoma (decreased Ach breakdown at M3--\>miosis--\>open Canal of Schlemm)

Answer 65

* "Long"-acting reversible AChE inhibitor * Use = tx of myasthenia gravis

Answer 66

* Reversible AChE inhibitor--\>increased stimulation of both nicotinic and muscarinic receptors * Use = Tensilon test (to dx myasthenia gravis or AChE overdosage) * Note: Tx overdoses of this or -stigmines with Atropine

Answer 67

* "tACh" * Reversible AChE inhibitor--\>increased nicotinic and muscarinic stimulation * Use = tx of Alzheimer's disease (slows progression by 6 months) * It works bc a decrease in Ach has been noted in AD * "Tacrine Alzheimer's Disease to slow it down"

Answer 68

* Inhibit AChE--\>increased stimulation of nicotinic and muscarinic receptors * Use = ophthalmic ointment that txs wide angle glaucoma (d/t increased M3 stimulation...) * "Echo in the eyes" * Systemic SE: seizures, bradycardia, flaccid paralysis

Answer 69

* "Mala = bad, and Para goes with mala" * Parathion/Malathion: * Poisons. * These, and the -phates, --\>szs, bradycardia, flaccid paralysis, death when give systemically

Answer 70

* Reverses AChE inhibitor binding to Ach--\>allows AChE to function normally again * Use = tx of organophosphate/AChE inhibitor poisoning * This is the ONLY med that reverses both the muscarinic AND nicotinic side effects of organophosphates!!! * (Atropine only reverses muscarinic side effects) * "Have a Parade because your AChE is back"...weeeaak

Answer 71

* Prevent serotonin reuptake--\>increased serotonin effect * Uses = major depression, OCD, anxiety disorders * SE = sexual dysfunction, and serotonin syndrome (muscle stiffness, hyperthermia, ANS instability)! * Serotonin syndrome occurs when SSRI is given with: * MAO inhibitor * TCA * Tramadol * Ondansetron * Linezolid * Triptans

Answer 72

Use = tx for serotonin syndrome (Cyp on serotonin)

Answer 73

* "ti-TBD" * Block 5-HT AND NE reuptake. * Also inhibit muscarinic, alpha-adrenergic, and histaminic receptors--\>many side effects! * Uses = tx of major depression, chronic pain * SE = sedation, postural hypotension/**wide QRS**/arrhythmias (MCC of death); anticholinergic effects (ABCDs); seizures * Trazadone--\>priapism * Risk of inducing mania in susceptible patients! * "Wide PPCAMSS" * **Tx of overdose = sodium bicarbonate!**

Answer 74

* Venlafaxine/Nefazodone--\>block NE/5-HT reuptake--\>tx depression * (Like TCAs) * Mirtazapine: inhibits alpha2 and 5-HT2 receptors--\>increased NE and 5-HT release * **Commonly used to tx depression in pts with insomnia** * Use =general anxiety disorder, depressive disorders * SE = sedation, increased appetite--\>wt gain

Answer 75

* Irreversibly bind MAO--\>increased levels of 5-HT, DA, and NE in the presynaptic neuron--\>leak out and activate receptors * (Bc irreversible, cant give SSRI for 2 weeks after D/C these) * Use = **atypical depression** (characterized by mood reactivity!) * SE = HTN crisis with tyramine-containing foods (wine, cheese...)

Answer 76

* **Inhibits MAO-B-**-\>increased DA in presynaptic neuron--\>decreased DA degradation * **Adjunct for PD** tx (parkinson's disease treatment)

Answer 77

* Inhibits IP3 second messenger cascade * Use = mood stabilizer for bipolar * SE = hand tremor, hypothyroidism, nephrogenic diabetes insipidus (d/t ADH antagonism) * Also teratogenic--\>Ebstein Anomaly (apical displacement of tricuspid leafs, decreased RV volume, RV atrialization)

Answer 78

* Block D2 receptors in CNS (and also inhibit H1 some) * Uses = tx positive sx of schizophrenia, delirium...Tourette * SE: (everything below) * Sedation (d/t H1 block) * Low potency--\>ABCCDSS (chlorpromazine, thioridazine) * Thioridazine--\>retinitis pigmentosa (Vision problems) * Chlorpromazine--\>Corneal deposits * High potency--\>Extrapyramidal side effects (especially haloperidol and fluphenazine) * Tardive dyskinesia = irreversible * Hyperprolactinemia--\>amenorrhea, galactorrhea * \*Neuroleptic malignant syndrome (muscle rigidity, fever, ANS instability...) * Tx for NMS = Dantrolene

Answer 79

* Block DA AND 5HT2 receptors in brain (and some other receptors--\>SE) * Use = tx positive AND negative sx of schizophrenia, bipolar; delirium tx * \*SE = mild weight gain (especially Olanzapine); hyperprolactinemia * \*Clozapine--\>agranulocytosis * (Drugs CCCrush Myelocytes and Promyelocytes") * So monitor WBC count * Risperidone = most likely to--\>tardive dyskinesia * These have fewer EPS and anti-cholinergic SE than typicals

Answer 80

* Allosterically activate GABA receptor--\>increase Cl ion flow--\>membrane hyperpolarization--\>decreased CNS activity * Uses = tx anxiety, status epilepticus, alcohol withdrawal ("szs"), insomnia * **1st line for status epilepticus!** * SE = sedation * \*Shorter acting--\>more addictive and increased withdrawal * \*Longer acting--\>increased daytime drowsiness and fall risk

Answer 81

* Competitive GABA antagonist * Use = tx of benzodiazepine overdose * "Treat Benzos with the Flu"

Answer 82

* Same MOA as benzos (allosteric binding to GABA receptors), but longer half-life (more residual hangover effect) * Uses = Sedative for anxiety/insomnia; mgmt of szs * Thiopental--very lipid soluble--\>rapid redistribution (muscle and fat), so used for anesthesia induction * Overdose--\>cardiac/resp depression (tx = Use dialysis/alkalinize urine) * May get withdrawal if become dependent

Answer 83

* **GABA receptor agonist (like benzos)--\>decreased CNS activity** * Use = short-term tx of insomnia (non-addictive!) * "zzz-olpidem" * **SE = hallucinations, mild anterograde amnesia**

Answer 84

* **Decreases Na/Ca flow** across membrane--\>decreased nervous system depolarizations * Uses = GTCS, partial szs, status epilepticus * "pHeNytoin--hyperplasia, nystagmus" * SE = **gingival hyperplasia,** nystagmus; drug-induced SLE. * Also teratogen--\>fetal hydantoin syndrome (decreased fetal growth, cardiac/palate defects) * (4 things)

Answer 85

* Blocks fast voltage-gated Na channels of presynaptic neuron--\>decreased glutamate/aspartate release * Use = epilepsy tx * SE = Stevens-Johnson syndrome

Answer 86

* MOA unknown, but does increase GABA * Use = GTCS/myoclonic szs (DOC), and absence szs (2DOC) * Also, treats mania of bipolar disorder * Note: myoclonic szs occur in morning and are triggered by decreased sleep * SE = hepatotoxic

Answer 87

* Decreases Ca currents in neurons * Use = tx of absence szs (DOC)

Answer 88

* Inhibits Na ion flow--\>hyperpolarization--\>decreased nerve activity * Uses = first-line for simple szs, complex partial szs, and GTCS * \*DOC for complex partial szs and for trigeminal neuralgia * \* * SE = agranulocytosis, aplastic anemia; hepatotoxic

Answer 89

* Block Na ion flow--\>hyperpolarization, and GABA agonist * Use = tx epilepsy and migraines * "Top = head (migraines)"

Answer 90

* Inhibits GABA reuptake--\>increasing GABA effect * Use = combotherapy for partial szs

Answer 91

* Irreversibly inhibits GABA transaminase--\>increased GABA levels in synapse (stopped breakdown) * Uses = tx infantile spasms (Viga"Baby"trin) * Or used as adjunct therapy for adults with refractory complex partial szs * SE = visual field constriction and even visual loss

Answer 92

* "Leave-tired-acetam" * "Leaves" * May bind synaptic vesicle proteins--\>interrupts nerve conduction * Uses = partial szs, myoclonic szs, GTCS * SE = drowsiness, depression * "Tired"

Answer 93

* Depolarizing NM blocker, competes with Ach to reversibly bind nicotinic receptors * Key points = depolarizing and reversible * Train-of-four response = phases * Phase 1--initial binding--\>Continuous depolarization * Phase 2 blockade--when the ion channel begins to repolarize but is desensitized d/t overstimulation * CAN use an AChE inhibitor to stop a Phase 2 block, but nothing can stop Phase 1 * Use = produce quick muscle paralysis for endotracheal intubation, or for emergency procedures * \*SE = hyperkalemia, cardiac arrythmias... * Malignant hyperthermia if given with halothane. Treat with dantrolene.

Answer 94

* Non-depolarizing NM blocker that competitively binds nicotinic receptors * Does not activate it (unlike succinylcholine) * Short-acting, easily reversible * Use = adjunct to general anesthesia induction * Train-of-four response = fading pattern (not phases) * SE = hypotension * Can reverse effects with AChE inhibitor (-stigmine)

Answer 95

* Block neuron Na channels--\>decreased activity * Use = local anesthesia * \*SE = seizures * Epinephrine (or other vasoconstrictors) are often given locally with the local anesthetic--\>decreased systemic absorption rate--\>more effective nerve block

Answer 96

* Directly activate GABA--\>decreased neuronal activity * Use = general anesthesia induction and maintenance * SE: myocardial and respiratory depression * Halothane--\>fulminant hepatic necrosis, cardiac arrhythmias * Methoxyflurane and enflurane--\>nephrotoxic * Halothane + Succinylcholine--\>malignant hyperthermia

Answer 97

SE: propofol--\>hypotension, o/w not very HY

Answer 98

* Bind/activate opioid receptors throughout nervous system--\>increased K efflux--\>hyperpolarization/decreased activity of neural cells--\>blocked pain transmission * Uses = pain control, cough suppression (codeine/dextromethorphan--\>suppress cough reflex in brainstem), diarrhea tx, acute pulm edema tx (morphine--\>decreased anxiety/preload) * SE = cardiac/resp depression, constipation, miosis * Also, tolerance and dependence development--\>nonfatal withdrawal

Answer 99

* Opioid receptor antagonists * Use = to tx opioid overdoses

Answer 100

* Opioid agonist with long half-life--\>helps ease withdrawal sx but no high given * Use .= drug tx programs

Answer 101

* Opioid with mixed agonist/antagonist activity at mu and agonist activity at kappa--\>hyperpolarization and decreased activity of neural cells * Use = severe pain, especially for migraines (intranasal), labor pain, or postop pain

Answer 102

* Weak opioid mu agonist--\>...--\>decreased neuron activity * Also inhibits NE and 5-HT reuptake * Use = tx of moderate/severe chronic pain * Tram-"Midol" (for pain) * SE = seizures * "Flopping on the tramtrack"

Answer 103

* **Inhibits Ca release from the SR of myocytes**--\>muscle relaxation * Use = tx of malignant hyperthermia (d/t general anesthetics) * Also used to tx neuroleptic malignant syndrome d/t haloperidol, levodopa, or metoclopramide * Note: both of the above have muscle breakdown, hyperthermia, etc * SE = hepatotoxicity

Answer 104

* Crosses BBB--\>DOPA-decarboxylase converts it into dopamine--\>increased CNS dopamine * Use = first line for Parkinson's * \*SE: dyskinesia/sporadic mvmts, cardiac arrhythmias (d/t peripheral conversion) * Also, get predictable wearing-off phenomenon and unpredictable "off/on" phenomenon * Don't take B6/multivitamin bc --\>increased levodopa peripheral metabolism

Answer 105

* Give with levodopa * Inhibits DOPA-decarboxylase in periphery--\>increased levodopa in CNS

Answer 106

* Partial DA receptor agonist * Use = PD adjunct; also helps with hyperprolactinemia * Other PD drugs are: * DA agonists (Amantadine) * MAO-B inhibitors (Selegiline)

Answer 107

* "Mem"-ory (related to AD) * \*NMDA receptor antagonist--\>decreased glutamate neuronal excitation--\>decreased CNS damage--\>AD sx improvement * **Use = severe AD (sx improvement only!)** * SE = agitation, H/A, dizziness (all CNS effects)

Answer 108

* Postsynaptic 5-HT1b-1d (serotonin) receptor agonists--\>decreased dura vasodilation/inflammation * Uses = acute migraines, cluster headaches * SE = coronary vasospasm (d/t 1b agonism) * So C/I in pts with CAD

Answer 109

* Bupropion = TCA, but is also a nicotinic antagonist * Verenicline = partial agonist/antagonist at a4b2 nicotinic receptors in brain * **SE= suicidality** * By binding nicotine receptors, these interfere with the smoking reinforcement/reward loop * Use = smoking cessation (and bupropion also is used for depression) * SE = bupropion--\>szs

Answer 110

* Presynaptic 5-HT1A receptor partial agonist * Use = for general anxiety disorder * No hypnotic, sedative, or euphoric effects (so low abuse potential!) * Onset of action can take several weeks * "Sara's anxious until she's on the Bus, but it takes a while to get here"

Answer 111

* "GABAPENtin = GABA analogue, postherpatic neuralgia, edema (SE), neuropathic pain" * GABA analogue * Use = **tx of postherpetic neuralgia, c**hronic neuropathic pain, and partial szs * SE = **peripheral edema**

Answer 112

* Binds Ca channels in CNS--\>decreased glutamate and NE release * Uses = fibromyalgia, chronic neuropathic pain * SE = dizziness

Answer 113

* "The Queen Proclaims Diso's Pyramid" * "Double Quarter Pounder" * Bind activated Na channels--\>block Na inflow in cardiac myocyte--\>prolong Phase 0--\>slowed conduction of action potential--\>slowed rate of cardiac muscle contraction * Delayed Phase 3 repolarization (K+ channel block somewhat)--\>prolonged QT--\>watch out for torsades * Uses = Afib, WPW syndrome, Vtach * SE = cardiac arrythmias (including torsades) * Quinidine--\>cinchonism * Procainamide--SLE * Use-dependent: 1C \> 1A \> 1B * (as ion channels depolarize more frequently, these become more effective)

Answer 114

* "Lettuce, Tomato, Mexico" * Bind activated AND inactivated Na channels--\>block Na inflow in cardiac myocyte--\>prolong phase 0 and shorten phase 3--\>decreased ability to stimulate contraction (bc can't get to peak) * Uses = ventricular arrythmias (Vfib and Vtach) * Lidocaine = DOC for prevention and **tx of post-MI arrythmias** * (B/c Class 1B is least-use dependent (better in ischemic myocardium))

Answer 115

* "Fries Please" * Bind activated Na channels--\>block Na inflow into cardiac myocyte--\>prolong phase 0 only--\>slowed action potential rate (but not duration)--\>slowed rate of contraction * Use = supraventricular arrhythmias * SE = life-threatening arrhythmias * Avoid in pts with structurally abn hearts (h/o CAD, low ejection fraction, etc) * "The fries are life-threatening" * The MOST use-dependent * (For example, --\>longer QRS during exercise, but nl QRS at rest)

Answer 116

* "AIDS" * Bind K channels--\>prolong phase 3 repolarization--\>long QT (and long action potential) * Long QT so may--\>torsades de pointes * Uses = atrial arrhythmias (Amiodarone and Sotalol also tx ventricular arrhythmias) * Amiodarone: * Actually Class 1-4 agent. * Side effects = pulmonary fibrosis, thyroid dysfunction, blue-grey skin discoloration * **(But don't usually get torsades with Amiodarone!)**

Answer 117

* Block voltage-gated Ca channels on cardiac myocytes and on SA and AV nodes--\>slow phase 4 spontaneous depolarization (= prolonged PR) and also delay repolarization (slowed HR) * Uses = supraventricular tachycardia (like Afib) * SE = heart block, constipation, gingival hyperplasia

Answer 118

* Increases K efflux in SA and AV nodes--\>hyperpolarization--\>less activation * Use = supraventricular tachycardias, and cardiac stress testing * DOC for paroxysmal supraventricular tachycardia * SE = flushing, dyspnea

Answer 119

Suppresses ectopic pacemakers (especially if d/t digoxin toxicity)

Answer 120

* Used to treat torsades * Used to tx digoxin toxicity

Answer 121

That they are the Class 2 anti-arrhythmics

Answer 122

* Inhibits Na/K pump--\>increased IC Na--\>decreased Na/Ca exchange--\>increased IC Ca--\>increased contractility * Also increases PSNS outflow at nodes--\>decreased HR * Use = tx for heart failure * **SE = blurry, yellow vision.** GI upset. ECG changes (long PR, short QT, ST scooping, T wave inversion) * Hypokalemia makes these side effects worse (bc K usually competes with Digoxin to bind Na/K pump) * Renal failure (decreased excretion) and quinidine (displaces Digoxin off albumin) also make the SE worse * Verapamil/Diltiazem can--\>digoxin toxicity by raising its levels * Digoxin toxicity: Tx with potassium and digoxin FAB (aby)

Answer 123

* Synthetic hBNP. Binds guanylate cyclase receptor--\>increased cGMP--\>smooth muscle relaxation/dilation--\>reduced preload and afterload * Use = rarely used for acute decompensated HF (doesn't help mortality) * SE = hypotension

Answer 124

* Converted to NO in the cell--\>stimulates guanylate cyclase--\>increased cGMP--\>inactivation of MLC--\>smooth muscle relaxation * Works mostly on smooth muscle of veins--\>decreased preload * It also relaxes the coronary artery smooth muscle * (This may be bad if +cardiac ischemia bc--\>coronary steal syndrome) * Uses = tx of angina, pulmonary edema, HF * SE = compensatory tachycardia, H/A, ortho hypotension, flushing * Need nitrate free interval daily to prevent tolerance * Amyl nitrite = DOC for cyanide poisoning * Isosorbide mononitrate--has highest oral bioavailability

Answer 125

* DOC for cyanide poisoning * (From the nitrate drug class)

Answer 126

Highest oral bioavailability of the nitrates

Answer 127

* IV only. * Converted to NO in the bloodstream--\>stimulates guanylate cyclase--\>inactivation of MLC--\>smooth muscle relaxation of peripheral veins AND arteries--\>reduced preload AND afterload * Uses - acute mgmt of a HTN crisis, severe HF, or cardiogenic shock * **DOC for most HTN emergency** * SE = cyanide toxicity * **(Tx with thiosulfate** (not amyl nitrate))

Answer 128

* DOC if pt has DM and HTN * Inhibit peptidyl dipeptidase (ACE)--\>decreased vasoconstriction, decreased aldosterone, etc--\>decreased bp and blood volume * Uses = HTN and CHF * Also used to tx and prevent diabetic nephropathy * Shown to decrease mortality in post-MI pts (bc decreased aldo--\>decreased cardiac remodeling) * SE = "CATCHH:" Cough, Angioedema, Teratogen (fetal renal malformation), Creatinine increase (decreased GFR), Hyperkalemia, Hypotension * Do NOT give if pt has bilat renal artery stenosis!

Answer 129

* Block AT (AT1) receptors--\>...--\>decreased bp and blood volume * Uses = HTN and CHF * Also used to tx and prevent diabetic nephropathy * Same side effects as ACEi, but no cough/angioedema

Answer 130

* Direct relaxation of arteriolar smooth muscle--\>decreased bp * Uses = HTN and HF (reduces afterload) * DOC for HTN in pregnancy **(ecclampsia, preecclampsia)** * SE = Drug induced lupus, reflex tachycardia, headache

Answer 131

* Direct relaxation of arteriolar smooth muscle * Uses = tx of refractory HTN * Also promotes hair growth

Answer 132

* Block voltage-gated L-type Ca channels--\>decreased Ca inflow--\>peripheral vasodilation * Uses = HTN, Prinzmetal angina, and Raynaud, **and DES** * DOC (or HCTZ) for isolated systolic HTN * Do not affect renal insufficiency

Answer 133

* "GUMI bear with bad heart and bad lungs in descending loop" * Act on PCT and descending loop of Henle--\>keep water in tubule--\>increase urine--\>decrease effective circulating volume * Uses = decrease intracranial or intraocular pressure by volume depletion * SE are b/c it initially causes expansion of circulating volume (before renal elimination): * Pulmonary edema * **C/I in pts with CHF**

Answer 134

* "Ascent-azolamide" * Inhibit carbonic anhydrase in PCT cells--\>less bicarb reabsorbed and more Na lost--\>increased renal H2O and electrolyte loss * CA also helps produce aqueous humor in the eye! * Uses: * alkalinize the urine prn after toxin ingestion, * treat glaucoma, * tx/prevent altitude sickness * SE = hyperchloremic metabolic acidosis, **hypokalemia, and hypocalcemia**

Answer 135

* **Sulfonamide derivative** that inhibits NA/K/2Cl in thick ascending limb--\>loss of water and electrolytes * No hyponatremia (no gradient there to reabsorb water in response to ADH) * Use = tx volume overloaded states a/w heart failure, liver failure, renal failure. * Also tx of HTN and hyperCa * SE = **hyperuricemia (--\>gout attack), ototoxic** * Allergic rxn in pts with sulfa allergy * Note: the hyperuricemia is bc of increased PCT Na reabsorption

Answer 136

* Diuretic, same MOA as loops, but **not sulfonamide-related.** * Give this in pts who cannot tolerate furosemide d/t sulfa allergies.

Answer 137

* Inhibit NaCl transporter in DCT--\>increased renal loss of H2O and salt * Uses = HTN, nephrogenic DI (decreases polyuria), and recurrent kidney Ca stones * SE = hypokalemia/hyponatremia and many hypers (hyperuricemia, hypercalcemia, hyperlipidemia) * The increased Ca can help with osteoporosis * DOC for essential HTN (without CHF or diabetes)

Answer 138

* Competitive aldosterone receptor antagonist--\>decreased Na and H2O reabsorption--\>decreased K excretion * Also is a competitive androgen receptor antagonist * Uses = tx primary hyperaldosteronism, HF volume overload, HTN * Also used to tx female hirsutism a/w PCOS * Bc it antagonizes aldosterone--\>decreased cardiac remodeling--\>decreased CHF mortality * SE = hyperkalemia, gynecomastia

Answer 139

Same as Spironolactone, but less anti-androgen effect--\>no gynecomastia

Answer 140

* Blocks Na channels in DCT--\>block Na/H2O reabsorption and therefore less K excretion * Uses = combotherapy to tx volume overload and HTN * SE = hyperkalemia

Answer 141

* Inhibit PDE5 (in cardiac/smooth muscle)--\>increased cAMP levels--\>opens Ca channels--\>Ca flows in--\>increased contractility * Use = tx of **acute decompensated HF** * SE = N/V * Note: increased cAMP also--\>vasodilation in smooth muscle (so can limit usefulness in hypotensive patients)

Answer 142

* Inhibits cGMP-specific PDE5 (in penis corpus cavernosum and pulm vasculature)--\>increased cGMP--\>smooth muscle relaxation--\>increased penis blood flow/erection and pulm vasodilation * Uses = erectile dysfunction, pulmonary arterial HTN * C/I in pts on nitrates d/t risk of life-threatening hypotension!

Answer 143

* Short half-life and rapid onset of action * Binds AT3--\>accelerates its action--\>degrades several clotting factors (especially thrombin) * Uses = acute tx for DVTs, pulmonary embolism, other thromboembolic events * Also used in tx of acute MI * SE = bleeding (tx with protamine sulfate, which inactivates heparin); HIT (d/t formation of anti-platelet abys) * Monitor effectiveness with PTT

Answer 144

Tx of bleeding caused by heparin | (Inactivates heparin)

Answer 145

* LMWHs. More active in degrading factor 10, less active in directly degrading thrombin * Longer DOA (so less frequent dosing)

Answer 146

* "You're Fond of it because it works even if you have HIT hx" * Binds AT3--\>accelerates its action in degrading factor 10a--\>inhibits coag cascade * Uses = Acute DVT or pulm embolism tx (especially in pts who have h/o HIT) * SE = bleeding

Answer 147

* Inhibits Vitamin K-dependent carboxylation of 2,7,9,10, C and S in liver * Long half-life; slow onset * Monitor PT * Uses = chronic anticoagulation in pts at risk for thromboembolism * SE = bleeding (tx with fresh frozen plasma (fastest) or Vitamin K (slower)); teratogen * Also can--\>skin necrosis (d/t transient hypercoagulation b/c protein C has shortest half-life and therefore goes away fastest) * Metabolized by p450 (drug interactions)

Answer 148

Tx of Warfarin-induced bleeding

Answer 149

* (argatroban, -gatrans, -irudins) * Directly inhibit thrombin by binding thrombin active site * Uses = acute and chronic anti-coagulation * **Argatroban--DOC to tx HIT** * SE = bleeding * PT and PTT are both increased

Answer 150

* Directly inhibit factor 5a * Uses = DVT prophylaxis, pulm embolism prophylaxis in pts with Afib * SE = bleeding * Can be used for anti-coagulation in heparin-allergic pts

Answer 151

* Irreversibly inhibits COX1 and COX2--\>decreased PG synthesis * Decreased PGE2--\>analgesia, decreased fever, and decreased gastric mucus (--\>ulcers) * Decreased PGI2 also--\>gastric ulcers * Decreased TXA2--\>decreased platelet aggregation * Uses = anti-platelet, anti-pyretic, analgesic, anti-inflammatory * SE = bleeding (especially GI), gastric ulcers, Reye syndrome, allergy * Overdose--\>respiratory and metabolic acidosis (Tx = NaHCO3 (to alkalinize urine--\>promotes excretion))

Answer 152

* Irreversibly inhibits binding of ADP to platelet P2Y receptor--\>decreased ADP-mediated platelet aggregation * This blocks the fibrinogen-platelet rxn--\>blocked platelet plug formation * Uses = tx acute coronary syndrome (along with aspirin) * Also used in pts undergoing placement of a coronary stent to prevent thrombosis * SE = bleeding * Ticlopidine--\>neutropenia * Metabolized by p450 to be activated * Suitable alternative to aspirin

Answer 153

* Same MOA as Clopidrogel. * Use = tx acute coronary syndrome along with aspirin in pts undergoing percutaneous coronary intervention * SE = bleeding * Less metabolization by CYP2C19--\>less genetic variability in platelet inhibition than with Clopidogrel

Answer 154

Same effect as other-grels, but reversible allosteric inhibitor to P2Y receptor.

Answer 155

* Inhibits platelet cAMP PDE3--\>increased cAMP--\>increased PGI2 synth and decreased TXA2 synth--\>vasodilation and decreased platelet agg/thrombi * Use - tx of **claudication** in pts with PAD

Answer 156

* Inhibits platelet/endothelial cell adenosine uptake--\>increased circulating adenosine--\>activates platelet adenylate cyclase--\>increased cAMP--\>increased PGI2 synth and decreased TXA2 synth--\>vasodilation, decreased platelet aggregation * Also, at high doses it inhibits cGMP PDE--\>increased cGMP--\>further vasodilation * Uses = pharm cardio stress tests; secondary prevention of stroke (if used with aspirin)

Answer 157

* "A and B -- bind 2b and 3a" * 2\*3 = abSIX * Bind G2b/3a platelet receptor--\>inhibit fibrinogen and vWF binding--\>decreased fibrinogen cross-linking--\>impaired platelet aggregation * Use = tx of acute coronary syndromes * SE = bleeding

Answer 158

For river blindness (Onchocerca volvulus)

Answer 159

* Mebendazole or Albendazole: * For whipworm (trichuris), hookworm, roundworm, and pinworm. * Albendazole: * For strongyloides, neurocystericosis, Echinococcus

Answer 160

For schistosomiasis, neurocystericosis

Answer 161

For hookworm, roundworm, and pinworm

Answer 162

For tapeworm infections

Answer 163

* In order for a drug to be eliminated by the kidney, it must be a polar molecule (not lipophilic): * Liver makes things polar through 2 sets of reactions: * 1. Phase 1 metabolism = Cytochrome p450 * Alters the drug to make it more amenable to combining with polar molecules. (Usually oxidation, reduction, or hydrolysis) * 2. Phase 2 metabolism = addition of polar moiety (sulfate, acetate, glucuronate) * Makes drug water-soluble and kidney can excrete it

Answer 164

* Promote conversion of plasminogen to plasmin--\>acts to degrade fibrin-\>degrades the thrombus * Give when emergent restoration of blood flow is essential * Indicated in : massive PE, stroke, and acute MI * SE = bleeding * C/I in pts with active bleeding, recent surg, or h/o hemorrhagic stroke * Most effective if given within a few hours of sx onset

Answer 165

* Inhibits plasminogen activation--\>inhibits fibrinolysis * Use = tx of post-surg bleeding and hemophilia * SE = thrombosis

Answer 166

* Stimulates BM to enhance erythroid proliferation and differentiation--\>increased hematocrit * Use = tx of anemia a/w chronic renal insufficiency, chemo, or critical illness * SE = cardiovascular events and thrombotic complications if used to increase Hb levels too much

Answer 167

* Lispro/Aspart: * Rapid onset (peak 1 hour); very short acting (3-4 hours) * Regular insulin: * Rapid onset (peak 2-3 hours); short-acting (5-7 hours) * Semilente: * Quick onset (peak 6 hours); intermediate-acting (10-12 hours) * Lente/NPH: * Intermediate onset (peak 10 hours); intermediate-acting (18 hours) * Ultralente/Glargine/Detemir: * Slow onset (peak 12 hours); long-acting (24 hours) * Glargine = longest and has no peak

Answer 168

* MOA: * 1. Inhibit K channel in beta cells--\>stimulate insulin release * 2. Prolong insulin binding to target receptors--\>increases insulin action on target tissues * 3. Increased insulin levels--\>inhibition of glucagon secretion--\>decreased serum glucagon levels * Use = DM2 tx * SE = hypoglycemia; disulfiram-like rxn with EtOH * \*C/I in pregnancy--cause insulin depletion in fetal pancreas * \*Excreted by liver/kidney (so be careful in pts with these problems)

Answer 169

* Inhibits hepatic gluconeogenesis and increases peripheral glucose use--\>decreased BSG * Use = DM2, polycystic ovarian syndrome * SE = GI upset; lactic acidosis * Kidney excretes it, so C/I in pts with renal problems * Does NOT cause hypoglycemia!

Answer 170

* Bind PPARgamma--\>upregulates genes and adiponectin--\>decreased insulin resistance * Takes a few weeks to start working since it is upregulating genes * Use = DM2 * SE = wt gain/edema; hypoglycemia

Answer 171

* Inhibit alpha-glucosidase (enzyme on brush border of small intestine)--\>less breakdown into monosaccharides--\>decreased absorption of postprandial carbs * Uses = DM2 tx (and can be used in combo with insulin in DM1) * SE = GI upset (flatulence, diarrhea)

Answer 172

* Bind K channel in beta cell (different binding spot than sulfonylureas)--\>insulin release * SE = wt gain; hypoglycemia

Answer 173

* Inhibit DPP4--\>GLP1 doesn't get degraded--\>increases insulin secretion and decreases glucagon secretion * SE = N/V

Answer 174

* Mimic GLP1--\>increased insulin secretion, decrease glucagon secretion * SE = wt loss

Answer 175

* Inhibit HMG-CoA reductase--\>decreased cholesterol synth * Also increase LDL receptor concentration on hepatocytes--\>decreased serum LDL * Use = decrease total cholesterol, and especially LDL, levels * SE = myopathy (and possible rhabdomyolysis); abn liver function tests; teratogen

Answer 176

* Decreases cholesterol absorption in small intestine * Also, bc this--\>decreased hepatocyte cholesterol stores, the hepatocytes upregulate LDL receptors--\>decreased LDL * Uses = adjunct to diet or other meds to tx hypercholesterolemia (high cholesterol, high LDL) * SE = myalgia; elevated liver function tests; steatorrhea

Answer 177

* = Bile acid-binding resins * Inhibit bile acid reabsorption in jejunum/ileum. This--\>lower levels of bile acids--\>increased conversion of cholesterol to bile acids--\>lower IC cholesterol--\>increased LDL receptors--\>decreased LDL * Use= to lower cholesterol/LDL * SE = **GI Upset/diarrhea; medication tastes bad;** ADEK decreased absorption... * "tastes like a tyr-ant" * Also, --\>hyperTG bc synth of TG also gets upregulated in liver * **So C/I if pt already has high TG!!**

Answer 178

* Stimulate LPL--\>TGs get broken down into chylomicrons and VLDL--\>then removed from circulation * Use = decrease TG levels (also mild LDL decrease and HDL increase) * SE = myositis (esp if given with statin); and liver function tests, **hepatotoxicity and gallstones** * Also, compete with Warfarin for binding sites on plasma proteins--\>effects of Warfarin may be increased

Answer 179

* Inhibit apolipoprotein A1 breakdown--\>increased HDL levels * And inhibits adipose tissue lipolysis--\>less precursors for VLDL and LDL production * And inhibits liver TG synth * Uses = increases HDL levels; also helps decrease cholesterol, LDL, and TG levels some * SE = flushing mediated by PGs (decreased by also giving aspirin); hyperuricemia--\>gout exacerbations; insulin resistance (so increase DM meds prn)

Answer 180

* Structural analogues of pyrophosphate--\>inhibits and "kills" osteoclasts--\>decreases osteoclastic bone reabsorption * Uses = prevention and tx of osteoporosis * Also used for Paget dz of the bone, bone metastasis a/w hypercalcemia * (3 things) * SE = GI upset (esp esophageal erosions); jaw osteonecrosis, Afib (3 things)

Answer 181

* Inhibit thyroid peroxidase--\>inhibit iodotyrosine coupling--\>decreased thyroid hormone synthesis and decreased T4/T3 conversion peripherally * Use = tx of hyperthyroidism * SE = **agranulocytosis**; hepatotoxic

Answer 182

* Is synthetic T4. * Use = tx of hypothyroidism * And used to suppress TSH secretion to tx goiters/thyroid cancers * Overdose--\>hyperthyroidism sx

Answer 183

* Binds tubulin--\>induces microtubule depolymerization--\>decreased WBC migration to affected site * Use = tx of acute gouty attack * SE = diarrhea

Answer 184

* Decreases reabsorption of uric acid in PCT by blocking active transport * Use = to prevent further gouty attacks; also, to prevent/tx hyperuricemia (like in tumor lysis syndrome)

Answer 185

* Inhibits xanthine oxidase--\>decreased conversion of xanthine to uric acid * Use = same as probenecid * SE = both Allopurinol and Probenecid can stimulate acute attacks at first or make acute attacks worse

Answer 186

* Mimic actions of endogenous glucocorticoids (vasoconstriction, stimulation of gluconeogenesis and protein catabolism, decrease circulating WBCs, inhibit phospholipase A2--\>decreased PG and LT formation, and stimulation of gastric acid and pepsin synth) * Uses = tx of adrenocortical insufficiency, allergic rxns, collagen-vascular disorders (RA, SLE, etc), inflammatory bowel disease, asthma, spinal cord compression...immunosuppression...etc * SE = Cushing syndrome sx (osteoporosis, irritable, hyperglycemia, fat redistribution). * Also impaired wound healing, PUD, muscle wasting...

Answer 187

* Inhaled glucocorticoid. * Use = tx of chronic asthma. * Make sure to do oral rinsing to prevent oral Candidiasis

Answer 188

* Both of these treat obesity * Orlistat: * Inhibits lipase--\>decreased intestinal fat absorption * SE = steatorrhea, decreased ADEK * Sibutramine: * NT (serotonin, NE, DA) reuptake inhibitor * Not really sure how this helps

Answer 189

* Inhibits release of many hormones, reduces GI motility, causes vasoconstriction * Uses: * 1. Tx of esophageal varices * 2. Tx of VIPoma diarrhea; tx of Zollinger-Ellison syndrome; tx of acromegaly...

Answer 190

3 effects: * 1. V1 receptors--\>vasoconstriction * 2. V2 receptors--\>increased collecting duct permeability to H2O * 3. V2-like--\>increased Factor 8 activity b/c increase vWF release from endothelial cells * Uses = tx of central DI; tx of septic shock and cardiac arrest; can also help with vWF dz or Hemophilia A before minor surg procedures * Also can help prevent wetting your pants/bedwetting * SE = hyponatremia...

Answer 191

* Made in posterior pituitary--\>stimulates uterine and breast contraction * Uses = induce labor; stimulate milk let-down * Also used to control postpartum uterine hemorrhage

Answer 192

* Competitive androgen receptor antagonist--\>decreased testosterone growth effects on prostate * Note: --\>increased LH levels d/t decreased inhibition by testosterone * **(So always give with Leuprolide)** * "F-Leu-tamide" * Use = tx of prostate cancer * SE = gynecomastia...

Answer 193

* Agonist at androgen and progesterone receptors--\>decreased LH and FSH secretion--\>decreased endometrium and breast growth * Use = tx endometriosis, hereditary angioedema * SE = androgenic SE in women (hirsutism, acne, etc)

Answer 194

* Inhibits 5-alpha reductase--\>decreased DHT--\>decreased prostate growth * Uses = tx of BPH, prostate cancer, and early male-pattern baldness

Answer 195

* Inhibits aromatase--\>decreased estradiol levels * Use = chemo agent for ER+ breast cancer * SE = osteoporosis; increased incidence of CV events in pts with pre-existing CAD

Answer 196

* Competitive ER antagonist. * But bc it is competitive, high estrogen amounts can overcome it, so it is most effective in postmenopausal women * Uses = chemo agent for ER+ breast cancer; can help with osteoporosis * SE = thromboembolism; endometrial cancer; hot flashes * Increased endometrial cancer risk bc it works as an agonist there (remember, it is a SERM)

Answer 197

* Mixed estrogen agonist/antagonist. * Use = osteoporosis tx (agonist), and to reduce risk of invasive breast (antagonist) cancer in **postmenopausal women** * Does NOT increase endometrial cancer risk * SE = thromboembolism

Answer 198

* GnRH agonist--\>initial LH/FSH release, but then down-regulation--\>decreased estrogen and testosterone * Uses: * If given continuously: tx of metastatic prostate cancer, leiomyomas * If given in pulsatile manner: tx of infertility

Answer 199

* Partial agonist at ER in the pituitary--\>decreased nl estrogen feedback inhibition--\>increased LH/FSH release--\>ovulation * Use = infertility tx in pts with ovulatory dysfunction (like in **PCOS)** * SE = hot flashes, abd discomfort, multiple pregnancies

Answer 200

* Mixtures of estrogen/progestin: * Synthetic progestin--\>decreased GnRH release--\>decreased LH and FSH * Low levels of synthetic estrogen--\>decrease FSH release and cannot stimulate LH release * Decreased FSH--\>inhibited follicle development * Decreased LH--\>no ovulation * Use = birth control... * SE = Increased thromboembolism risk (especially in women \> 35 who smoke) * Also, decrease ovarian and endometrial cancer risk

Answer 201

No increased thromboembolism risk

Answer 202

* High doses of progestins * Can take up to 72 hours after intercourse to inhibit ovulation

Answer 203

* Steroid compound. * **Competitive receptor antagonist** at progesterone receptor. * Use = abortifacent at high doses (--\>endometrial lining breakdown and cervical dilation) * "My feet press (on the progesterone receptor)"

Answer 204

* Weak bases (form salt and H2O upon rxn with HCl)--\>increase pH--\>reduce gastric acidity. * Also, may decrease pepsin activity bc pepsin is inactivated at pH \> 4 * Uses = GERD tx; also promote healing of duodenal ulcers

Answer 205

* Promote healing of duodenal ulcers by binding/providing physical protection to mucosal barrier * Requires acidic environment to be activated (don't take with antacids, H2 blockers, PPIs...)

Answer 206

* Reversibly block H2 receptor on parietal cells--\>decrease cAMP--\>decrease H/K pump--\>decreased gastric acid secretion * Uses = GERD tx, PUD... * SE = gynecomastia, p450 inhibition

Answer 207

* Irreversibly inhibit H/K pump in parietal cells--\>decreased HCl secretion * Uses = tx of PUD, GERD, ZE syndrome * Also help tx H pylori infection

Answer 208

* Blocks 5HT3 receptors in GI tract and in CTZ--\>inhibits activation of the vomiting reflex path * Uses = tx of N/V a/w chemo or surg

Answer 209

H1 receptor antagonist. Blocking GI H1 receptors--\>decreased GI motility--\>less N/V

Answer 210

* D2 antagonist in CTZ--\>blocks vomiting reflex * Also, stimulates gastric and small intestinal motility * Uses = tx diabetic gastroparesis, and an anti-emetic * \*SE = sedation, EPS

Answer 211

Similar to Metoclopramide, but does not affect GI motility (D2 antagonist in CTZ--\>blocks vomiting reflex)

Answer 212

* Irritants/stimulants = Castor oil, senna * Bulking agents = Lactulose, Sorbitol, Polyethylene glycol, Mg salts * Stool softeners (get emulsified in stool)= Docusate, mineral oil * Uses = tx constipation, and for bowel preparation for colonoscopies * Note: lactulose--also helps tx hepatic encephalopathy by being degraded by gut bacteria into compounds that promote nitrogen excretion

Answer 213

* Diphenoxylate and Loperamide: * Activate mu2 opioid receptors in gut--\>inhibit Ach release--\>decreased peristalsis * Pepto-Bismol: * Binds E coli toxins, stimulates fluid absorption, and more * Uses = tx of diarrhea sx

Answer 214

* Bacteria in gut break this down into sulfapyridine and aspirin * Aspirin acts as anti-inflammatory (inhibits COX) * Uses = inflammatory bowel disease (or RA or juvenile arthritis) * Do not give with folic acid (bc **sulfapyridine inhibits folate absorption)**

Answer 215

* Inhibits HMG-CoA reductase, decreases cholesterol absorption, and inhibits secretion of cholesterol into bile * (So inhibits cholesterol gallstones in 3 ways) * Uses = tx of primary biliary cirrhosis, or tx of cholesterol gallstones (alternative to cholescystectomy)

Answer 216

3 MOA: * 1. intercalate in DNA--\>block DNA and RNA synthesis * 2. Produce free radicals--\>membrane damage * (--\>dose dependent cardiac damage (so keep lifetime dose down!!!)) * 3. Disrupt fluid and ion transport across membranes * Doxorubicin: * For solid tumors, heme malignancies (acute leukemia, acute lymphoma, multiple myeloma), Kaposi sarcoma * Daunorubicin: * For acute leukemia (AML, ALL, CML) and neuroblastoma * Idarubicin: * For AML * SE = cardiac toxicity (DCM), BM suppression * Give Dexrazoxane to decrease free radical formation--\>decreased heart toxicity

Answer 217

Decreases the free radical formation caused by the **anthrocyclines (-rubicins)--\>less heart toxicity**

Answer 218

* Intercalates--\>inhibits DNA-dependent RNA polymerase--\>impaired RNA synthesis * Uses = adjunct for Wilms tumor or Ewing Sarcoma * SE = BM suppression * Plicamycin--used more for testicle cancers or Paget dz of the bone

Answer 219

* "Blee makes you free when you pee" * Binds DNA--\>triggers free radical formation--\>strand breaks/DNA synth inhibition * Uses = chemo for testicular tumors (and some more) * SE = pulmonary fibrosis; rare myelosuppression * Cell-cycle specific (--\> accumulation of cells in G2 phase)

Answer 220

* **Alkylating agent**--\>cross-links DNA--\>damages DNA * Uses = **CML** tx * (And in combo with other drugs for BM ablation before BM transplant) * SE = **pulmonary fibrosis** (and some more)

Answer 221

* "Rule of twos" * p450 activates it--\>alkylating agent--\>DNA cross-links--\>decreased DNA and RNA synth * Also, it suppresses B and T cell function * Uses = chemo for solid and heme malignancies * Also, immunosuppression for RA, SLE... * SE = hemorrhagic cystitis (prevent with fluids and MESNA); BM suppression

Answer 222

* **Alkylating** agents--\>cross-link DNA--\>inhibit DNA and RNA synthesis * Uses = tx of **brain tumors** (and some more) * Highly lipid-soluble and cross BBB!!

Answer 223

* Alkylating agent--\>cross-links DNA--\>decreased DNA and RNA synthesis * Uses = GU tumors mostly * SE = nephrotoxicity, otoxicity * (Have "plates in your ears and kidneys") * Mitigate nephrotoxicity by using Amifostine (scavenger of free radicals) * Skipped Mitomycin

Answer 224

Used to mitigate Cisplatin/Carboplatin nephrotoxicity

Answer 225

* **= preferred first-line dz modifier for severe RA** * Inhibits DHFR--\>decreased FH4--\>decreased thymidylate--\>decreased DNA synth * Uses: * 1. Chemo for various malignancies * 2. Immunosuppressant for autoimmune disorders (RA, Crohn, etc) * 3. Abortifacent when given with PG (tx small **ectopic pregnancies** or missed abortions) * SE = BM suppression; hepatotoxicity; teratogen; pulmonary toxicity

Answer 226

* Often given with MTX to minimize BM suppression * Gets converted to TH4 (downstream of MTX block), so it bypasses the inhibited enzyme

Answer 227

* HGPRT converts it into thio-IMP--\>acts as purine analogue--\>inhibits purine synthesis through feedback inhibition of several enzymes involved in de novo purine synthesis * Uses: * 1. Chemo, esp for **ALL** * 2. Immunosuppressant for IBD and psoriasis * SE = BM suppression * **Metabolized by xanthine oxidase** * Allopurinol inhibits xanthine oxidase, so if given with 6-MP then 6-MP levels increase!!--\>increased toxicity!

Answer 228

* Analogue of 6-MP. Converted to 6-MP in cell. * Uses = immunosuppressant for autoimmune dzs (SLE, etc)

Answer 229

* Converted into 5-FdUMP--\>inhibits thymidylate synthase--\>decreased thymines--\>disrupted DNA synthesis * Uses = Chemo for adenocarcinomas (especially of the colon) * "Flower in your colon" * SE = BM suppression, photosensitivity, mucosal ulcers * "Flower in your eye and mouth" * Cell-cycle specific (acts during S phase) * Note: see Note card 197 to see how this correlates with MTX and Leucovorin!!! * Giving Leucovorin makes MTX less toxic, but it makes 5-FU more toxic

Answer 230

* Converted in cell to araCTP--\>competitively inhibits DNA polymerase--\>impaired DNA synthesis * Uses = for AML and lymphomas * SE = BM suppression with pan"cyt"openia * Cell-cycle specific for S phase

Answer 231

* Inhibits topoisomerase 2--\>DNA strand breaks * Uses = tx of solid tumors like small cell lung carcinoma * SE = BM suppression * Cell cycle-specific for late S-G2 phase

Answer 232

* Binds tubulin--\>depolymerization of mitotic spindle--\>can't get past metaphase--\>decreased cell proliferation * Vincristine--used for ALL, lymphomas (part of MOPP for Hodgkin) * SE = peripheral neuropathy, BM suppression is rare!!! * "Christine's got nerve!" * Vinblastine--testicular cancer, lymphomas... * SE = BM suppression * "Blast the balls and the bone" * Cell cycle-specific for M phase

Answer 233

* "Stable taxi" * Bind tubulin--\>makes complex that **promotes stabilization** and polymerization of the mitotic spindle--\>halt of mitosis during metaphase * Uses = **ovarian and breast cancer...** * Also used to coat coronary artery stents to prevent restenosis * SE = BM suppression

Answer 234

* Inhibits ribonucleotide reductase--\>can't turn riboNT into deoxyriboNT--\>decreased DNA synthesis * Uses = tx for Myeloproliferative orders (CML, polycythemia vera) and melanoma * "MM hydroxyurea" * Also helps tx SCD bc it increases HbF * SE = BM suppression * Cell cycle-specific for S phase

Answer 235

* Inhibits adenosine deaminase--\>decreased purine degradation * Tx for hairy cell leukemia * "Five hairs"

Answer 236

* Monoclonal aby against HER2/neu (erb-B2) receptor--\>less uncontrolled cell growth * Uses = HER2+ breast cancer * SE = cardiac toxicity

Answer 237

* Competitive inhibitor of tyrosine kinase enzymes in abl, c-KIT, PDGF-R, etc * Uses = tx of CML, GISTs, and brain tumors

Answer 238

* "Renal failure, Infusion rxn, Twenty (CD20)---\>B cell lysis" (RITuximaB) * Monoclonal aby against CD20 (on B cells)--\>B cell lysis Uses: * 1. Tx of non-Hodgkin lymphoma and CLL * 2. Also used to tx autoimmune disorders (RA especially) * SE = infusion rxn; acute renal failure d/t tumor lysis syndrome * Prevent the infusion rxn by giving anti-histamine and Tylenol 30 minutes prior to admin

Answer 239

* Reversible COX1 and 2 inhibitor--\>decreased PG synth * Decreased PGE2--\>analgesia, lower T (anti-pyretic), and decreased gastric mucous * Decreased PGI2--\>increased gastric acid (--\>ulcers) * Uses = anti-fever, analgesic, anti-inflammatory * Indomethacin--also for gout, closing PDA * SE = GI bleeds, interstitial nephritis * Does NOT have significant anti-platelet effect (bc is reversible so platelets can replenish TXA2)

Answer 240

* ("select COX 2") * Irreversibly inhibits COX2--\>decreased PG synthesis * Note: COX2 is upregulated at sites of inflammation (like joint), COX1 is present in most tissues (stomach) * So this medicine minimizes gastric ulcers and other SE by leaving COX1 untouched * Uses = RA, OA, and other acute pains * SE = GI upset, interstitial nephritis; increased thrombosis risk

Answer 241

* Reversibly inhibits COX1 and 2 in the CNS--\>decreased PGE2 in CNS--\>decreased pain and temp * (It is mostly inactive in periphery, so minimal anti-inflammatory effects!!) * Uses = anti-pyretic and analgesic * SE = fatal hepatotoxicity with overdose * (Acetylcysteine = antidote)

Answer 242

* Antidote for Acetominophen overdose: * Contains SH groups which bind and inactivate Tylenol's toxic byproducts * Also helps CF pts by cleaving S-S bonds in mucus

Answer 243

* Reversible inhibitor of cysteinyl LT-1 receptor--\>blocks LTC4-E4 binding--\>decreased bronchoconstriction and decreased mucus * Uses = preventative tx of asthma (chronic asthma prophylaxis) * Zafirlukast inhibits P450

Answer 244

* "Zilch--LTs all gone" * Inhibits 5-lipoxygenase--\>decreased LTA4--\>decreased LTB4--\>decreased neutrophil chemotaxis--\>decreased airway inflammation * Note: LTA4 is what all of the LTs come from * Uses = chronic asthma prophylaxis (same as -lukasts)

Answer 245

Inhibits mast cell degranulation--\>less histamine--\>anti-inflammatory effects--\>prevents asthma exacerbations associated with allergens or exercise

Answer 246

* "Cyclops don't have IL2 eyes" * Inhibits calcineurin in T cell--\>decreased IL2 transcription--\>decreased IL2--\>decreased T cell activation--\>decreased production of other cytokines * "Decreased T cells--"T is for Transplant"" Uses : * 1. Immunosuppression in **transplant pts** * **2. Tx of GVHD** * 3. Tx of autoimmune dzs (like RA) * \*SE = nephrotoxicity; hepatotoxicity... * (Most SE are dose-dependent) * Metabolized by p450 (CYP3A4)

Answer 247

* Binds FKBP--\>Inhibits calcineurin--\>decreased IL2--\>decreased T cell activation * Use = immunosuppression in transplant pts * \*SE = increased infection risk; nephrotoxic; neurotoxic * Metabolized by p450 * So very similar to cyclosporine (except SE profile)

Answer 248

Similar to Tacrolimus, but inhibits mTOR--\>decreased T cell proliferation

Answer 249

* Acts in B and T cells to inhibit inosine monophosphate (IMP) dehydrogenase--\>decreased GMP in de novo purine synth--\>decreased DNA synth in B and T cells--\>decreased prolif of B and T cells * Use = immunosuppressant in transplant pts, also for autoimmune disorders

Answer 250

* alpha--made by WBCs * beta--made by fibroblasts * gamma--made by CD4 T cells * Produced in response to viral infection. * Have multiple actions to boost immune system in viral infection. * \*IFNa--tx of HBV and HCV; also tx of some cancers * IFNb--tx of MS (reduces exacerbations) * IFNgamma--tx of chronic granulomatous disease\*

Answer 251

Alprostadil: PGE1; relaxes smooth muscle and vasodilates Use = For ED and maintaining PDA "A" for PD'A' Misoprostol: PGE1; increases uterine contractions; inhibits HCl secretion and increases mucus in stomach Use = Prevents NSAID-induced gastric ulcers Also abortifacient when given with MTX Latanoprost: PGF2; increases aqueous humor drainage Use = Tx of chronic glaucoma Dinoprostone: PGE2; increases uterine contractions Use = Abortifacient Carboprost: PGF2; increases uterine contractions Use = Abortifacient

Answer 252

* It's a "PGI2 Pah-TIE" * Inhibit platelet aggregation and produce vasodilation (both by increasing cAMP) * Uses = tx of pulmonary arterial HTN

Answer 253

* "Intercepts TNFalpha" * Inhibits binding of TNFa and TNFb to their receptors--\>decreased TNFa effects--\>less release of other cytokines (IL1, IL6, IL8) is stimulated * Uses = autoimmune diseases (RA, etc) * SE = URIs...

Answer 254

May be used to tx RA

Answer 255

* "Inflicts pain on TNFalpha" * Really very similar to Etanercept, but this actually binds TNFalpha itself * Chimeric aby that binds TNFa--\>inhibits binding of TNFa with its receptor--\>decreased other cytokines released--\>anti-inflammation * Uses = autoimmune diseases (RA, IBD, etc) * SE = increased infection susceptibility * Adalimumab--same really, just monoclonal not chimeric

Answer 256

* (Just need to straight up memorize this one) * Decreases TNFa production--\>anti-inflammatory * Uses = tx of erythema nodosum leprae; also tx of multiple myeloma * C/I during pregnancy: * Causes phocomelia (shortening or absence of limbs)

Answer 257

* Block H1 receptors--\>bronchodilation, decreased pruritis, vasodilation, decreased GI motility, etc * Also has anti-cholinergic and anti-adrenergic effects--\>SE profile * Uses = tx of urticaria, allergic rhinitis, allergic rxns, motion sickness, sleep aid * Also used to tx acute dystonia (like from typical antipsychotics) * Promethazine--anti-emetic * Meclizine--motion sickness tx * SE = sedation; anticholinergic effects (ABCCDSS)

Answer 258

* Block H1 receptors--\>same effects as first gen * Uses = tx of allergic rhinitis and seasonal allergies * Less sedation than Diphenhydramine bc does not cross BBB * Minimal side effects

Answer 259

* "The lungs 'phylline' up, the heart 'phylline' bad" * Inhibits 'P'DE--\>increased cAMP--\>bronchodilation * Uses = tx of acute and chronic asthma * SE = cardiac arrhythmias, SEIZURES AND abd pain/N/V * (Happen bc theophylline has a very narrow therapeutic index) * Metabolized by p450

Answer 260

* --\>secretion of less viscous mucous in bronchi--\>thinner phlegm which helps stimulate resp tract secretion flow * Use = expectorant to get phlegm out

Answer 261

* Competitively inhibit endothelin receptors--\>pulmonary vasodilation * Use = tx of pulmonary arterial hypertension * SE = hepatotoxicity; teratogen

Answer 262

* Enhances flow of CL ions through GABA channels--\>increasing inhibitory effects of GABA * (Just like benzos and barbiturates it seems) * Use = tx of ethylene glycol or methanol overdose * (Acts as competitive substrate at the enzymes that produce the toxic metabolites from the other two) * SE = CNS depression; GI inflammation; teratogen

Answer 263

* Used in tx of alcohol cessation. * Inhibits acetaldehyde dehydrogenase--\>increased acetaldehyde when drinking (toxic)--\>N/V--\>incentive not to drink

Answer 264

Antidote = De"fero"xamine

Answer 265

Antidote = Calcium EDTA; dimercaprol; penicillamine

Answer 266

Antidote = Dimercaprol; penicillamine

Answer 267

Antidote = Sodium thiosulfate; nitrites

Answer 268

Antidote = 100% oxygen

Answer 269

* Actually Class 1-4 agent. * Side effects = pulmonary fibrosis, thyroid dysfunction, blue-grey skin discoloration * (But don't usually get torsades with Amiodarone!)

Answer 270

* Tx of ethylene glycol overdose * Inhibits alcohol dehydrogenase (unlike disulfiram)--\>decreased breakdown of ethylene glycol into toxic metabolites

Answer 271

* Lower triglycerides a lot * Raise HDL and LDL a little * If belch--\>bad fishy taste in mouth

Answer 272

* 2nd line for malaria, also 2nd line for RA * Metabolites build up--\>inhibit sphingomyelinase (like Niemann-Pick) so do eye exams periodically (remember cherry red macula)