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GER MS2 Unit 2 > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Bethanechol (Urecholine)

A
  • direct acting carbamic ester
  • direct acting muscarinic cholinomimetic
  • used for post op and neurogenic ileus, urinary retention
  • side effects: SLUDGE
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2
Q

Muscarine

Pilocarpine (Salagen)

Cevimeline (Evoxac)

A
  • direct acting non-ester alkaloid
  • direct acting muscarinic cholinomimetic
  • side effects: SLUDGE
  • pilocarpine: treats glaucoa
  • cevimeline: treats dry mouth
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3
Q

Nicotine (NRT)

A
  • direct acting non-ester alkoloid
  • direct acting nicotinic cholinomimetic
  • used for smoking cessation (reduces cravings)
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4
Q

short acting AChE inhibitors (0.5-2 hrs)

A
  • indirect acting carbamates; dock like ACh to temporarily inhibit
  • side effects: SLUDGE, general increase in cholinergic neurotransmission; paralysis
  • neostigmine (prostigmin): post operative and neurogenic ileus, urinary retension, myasthenia gravis, reversal of neuromuscular blockade
  • physostigmine (eserine): treats glaucoma
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5
Q

Donepezil (Aricept)

A
  • indirect acting non-ester
  • AChE inhibitor
  • treats Alzheimer’s (amplifies endogenous ACh in brain)
  • side effects: SLUDGE, general increase in cholinergic neurotransmission, paralysis
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6
Q

Edrophonium (Enlon)

A
  • indirect active non-ester
  • AChE inhibitor (v. short acting 5-15mins)
  • used to diagnose myasthenia gravis (deficiency vs. ACh crisis); treats ileus
  • side effects: SLUDGE, general increase in cholinergic neurotransmission, paralysis
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7
Q

Echothiophate (Phospholine)

A
  • indirect acting organophosphate
  • long acting ACh inhibitor (>100 hrs)
  • treats glaucoma
  • side effects: SLUDGE, general increase in cholinergic neurotransmission, paralysis
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8
Q

Pralidoxine (Protopam)

A
  • strong nucleophile that regenerates phosphorylated AChE
  • treats poisoning by nerve gas, insecticide; give for overdose of any indirect acting muscarinic
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9
Q

Sarin

Parathion

A
  • very potent indirect acting organophosphate
  • AChE inhibitor (forms covalent bond with receptor)
  • side effects: SLUDGE, general increase in cholinergic neurotransmission, paralysis; death
  • treat with pralidoxime and atropine before aging
  • sarin: volatile nerve gas
  • parathion: insecticide
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10
Q

tertiary amine antimuscarinics

A
  • block muscarinic receptors
  • side effects: general block of muscarinic functions
  • atropine: mydriasis, cycloplegia
  • scoploamine: prevent/reduce motion sickness
  • tropicamine: myrdiasis, clycloplegia (rapidly metabolized)
  • tolterodine (detrol): transient cystits, post op bladder spasms, incontinence
  • benztropine: treat maniestations of parkinson’s (crosses BBB)
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11
Q

quaternary amine antimuscarinic

A
  • blocks muscarinic receptors
  • side effects: general block of muscarinic functions
  • glycopyrrolate: reduces transient hypermotility (crosses membranes poorly)
  • ipratropium (atrovent): bronchodilation in asthma/COPD
  • tiotropium (spiriva): bronchodilation in asthma/COPD; longer acting that ipratropium
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12
Q

Hexamethoium (Methium)

Mecamylamine

A
  • ganglionic blocker; competitively inhibits Nn receptor and sympathetic tone
  • treats: HTN crisis; “bloodless” field surgery
  • rarely used
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13
Q

Succinylcholine (Anectine)

A
  • depolarizing blocker (MC used); overstimulates N receptor→ desensitization of muscle unit to further ACh (flaccid paralysis in 1 min)
  • used for brief procedures (tracheal intubation, dislocation resets)
  • side effects: respiratory paralysis, disturbance of autonomic function
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14
Q

Tubocurarine (Curare)

Mivacurium (Mivacron)

A
  • nondepolarizing blocker; blocks nicotinic (Nm) receptor
  • muscle relaxant or surgery without deep anesthesia
  • side effects: respiratory paralysis, disturbance of autonomic function
  • tubocurarine: lasts 30-60 mins
  • mivacurium: short acting (rapidly hydrolyzed)
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15
Q

Botulinum A toxin (Botox)

A
  • local paralytic; blocks vesicle fusion and ACh release on presynaptic terminal by degrading SNAP-25
  • treats achalasia, strabismus, oromandibular dystonia; reduces wrinkles
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16
Q

hyperbaric oxygen

A
  • prevents lipid peroxidation and delayed nerologic sequelae in CO poisoning
  • use in high risk individuals after smoke inhalation ( >30 y.o and/or loss of consciousness)
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17
Q

nitrites

A
  • turns RBC Hb→ metHb, CN moves Fe3+ on cyt to those in RBCs creating cyanometHb
  • dangerous for use with concurrent CO poisoning
  • patients who are G6PD deficiency will not respond to this treatment
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18
Q

sodium thiosulfate

A

enhances normal metabolism of cyanide via rhodanase

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19
Q

hydroxycobalamin (cyanokit)

A
  • binds with cyanide→ cyanocobalamin (B12)
  • treats smoke inhalation victims not improving with supportive care; cyanide exposure; nitroprusside at risk patients
  • give concurrently with sodium thiosulfate
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20
Q

methylene blue (urolene blue)

A
  • cofactor of NADPH reductase (gains e and donates it to reduce metHb)
  • treats methemoglobinemia >20-30% or with symptoms
  • side effects: hemolytic anemia (weak oxidizing capability); pain at injection site, dyspnea, reslessness, tremor
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21
Q

norepi (levophed)

A
  • nonselective agonist; α1, α2, β1
  • treats acute hypertension
  • side effects: HTN, arrythmias, headache
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22
Q

epi

A
  • neurohormone (no synapse)
  • nonselective agonist; α1, (α2), β1, β2
  • treats anaphylactic shock; + local anesthetics for dental procedures (less dramatic effect on BP, less irritating, and more potent than NE); glaucoma
  • side effects: palpitations, arrythmias, headache
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23
Q

amphetamine

A
  • indirect acting (increases release of norepi)
  • treats ADHD, narcolepsy; just for funsies
  • side effects: HTN, insomnia, anxiety, arrythmias
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24
Q

isoproterenol

A
  • nonselective β agonist (β1, β2)
  • treats shock, heart block
  • side effects: palpitation, tachy, headache
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25
dobutamine
* β1-selective agonist * treats cardiac decompensation, shock, heart block; **used as chemical cardiac stress test** * side effects: tachyarrythmias, HTN
26
albuterol (proventil) terbutaline (brethine)
* β2-selective agonist * prevents/reverses exercise-induced bronchospasm; treats mild asthma, COPD * **terbutaline: treats early labor** * side effects: can mask progressively severe inflammation; tachycardia, muscle tremor * takes 10-15 mins to act with 6-12 hrs duration * nebulizer delivers more but there are greater side effects; oral is least effective (requires more dose→ side effects)
27
phenylephrine (neo-synephrine)
* α1-selective agonist * treats nasal congestion, posterural hypotension * side effects: HTN, reflex brady; **desensitize receptors with overuse→ rebound congestion**
28
clonidine (catapres)
* α2-selective agonist (CNS) * treats HTN, shock, withdrawal from drug dependence * side effects: sedation
29
α-methyldopa (Aldomet)
* prodrug crosses BBB, metabolite (a-methylnorepi) activates CNS α2 * treats HTN * side effects: sedation
30
fenoldopam (corlopam)
* **selective dopamine agonist (D1 only)** * increases blood flow at renal, mesenteric, and cerebral arteries * 10 min half life **(good for HTN emergencies)**
31
dopamine
* mixed acting (direct/indirect) agonist: D1, α1, β1 * **Low dose: direct @ D1; treats renal failure** * **Medium dose: direct @ β1, some indirect; treats shock** * **High dose: direct @ α1**, some indirect; **vasoconstriction (treats HTN)**
32
phentolamine (regitine) phenoxybenzamine (dibenzyline)
* nonselective α-antagonists * treats **pheochromocytoma (during surgery** because trauma→ high catecholamines), **Raynaud's, frostbite** * side effects: postural hypotension, inhibits ejaculaton * **phenoxybenzamine:** also is a non-competitve blocker (covalently bonds to receptors)
33
pra**zosin** (minipress) tera**zosin** (hytrin)
* α1-selective antagonists * treats primary HTN, BPH (decrease resistance to urine outflow) * side effects: postural hypotension (usually 1st dose); less side effects than the nonselective α antagonists
34
1st generation nonselective β-antagonist
* **propranolol (inderal):** angina, HTN, arrythmias, migrains, anxiety * **timolol (betimol):** glaucoma * side effects: bradycardia, bronchoconstriction, sexual dysfunction * **do not use for CHF**
35
2nd generation β1-selective antagonist
* treat HTN, angina, arrythmias, **CHF** * side effects: brady, sexual dysfunction; less danger of precipitating an asthma attack than nonspecific β antagonists * **metoprolol (lopressor)** * **atenolol (tenormin)** * **bisoprolol (zebeta)**
36
3rd generation β-antagonists
* class A (nonselective; also α1 blocker) * **carvedilol (coreg)** * **labetalol (trandate)** * class B (β1 selective; also Ca2+ channel blocker) * **betaxolol (kerlone)** * ​treat CHF, HTN * side effects: brady, fatigue
37
tyramine
* indirect acting agonist; increases cytoplasmic NE release (MAO inhibitor) * invovled with an exchange transporter (tyramine in, NE out) * injections→initial BP spike due to NE release then acute tolerance when small cytoplasmic pool of NE is used up with repeat injections
38
Guanethidine (Ismelin)
* nerve ending blocker; false NT preferentially taken up by uptake1→vesicles fill with guanethidine; "shoot blanks" * treat HTN * side effects are many and serious (dont use in US, doesn't cross BBB)
39
cocaine
* prevents NE reuptake * used as a local anesthetic, nasoconstrictor * side effects: insomnia, anxiety, arrythmias
40
reserpine
* nerve ending blocker; release of empty vesicles (NE not taken into vesicles because it binds uptake1 and stops) * older anti-HTN * many serious side effects (esp. depression and suicide) * cheap, used abroad
41
α-me-tyrosine (Metirosine)
* nerve ending blocker; inhibits tyrosine hydroxylase (decreases NE and DA synthesis) * treats pheochromocytoma * many serious side effects
42
ephedrine (pretz-D)
* Mixed agonist: direct (β2) and indirect * treats nasal decongestion * side effects; anorexia
43
quinolone derivatives
* prophylaxis, treatment of acute malarial attacks * accumulate in parasite’s food vacuole, disrupt heme polymerization to hemozoin→ oxidative damage to membranes and digestive proteases * **quinine (qualaquin):** can also cause cinchonism, hypotension, hypoglycemia, abortion, arrhythmias * **chroloquine (aralen):** can also cause itching (Africans), retinitis (rare) * **hydroxyclhloroquine (plaquenil)** * **mefloqine (lariam)**
44
amantadine (symmetrel)
**+charge helps chloroquine overcome chloroquine-resistant malaria vacuoles;** point mutations against amantadine return bacteria to chloroquine-sensitivity
45
artesunate artemether
* artemisinin compound * specifically and selectively inhibit SERCA of P. falciparum * **artesunate:** neurotoxicity, long QT
46
atovaqunoe (mepron)
* nepthalene; depolarizes parasitic mitochondria and inhbits e-transport * antimalaria * used in combination with chloroguanide for chloroquine resistant strains of p. falciparum
47
chloroguanide/proguanil (malarone)
* antifolate; DHFR inhibit (human and parasitic pathway) * antimalarial
48
tetracycline clinamycin doxycycline
* antibiotics uses to treat severe malaria and chloroquine-resistant uncomplicated malaria * inhibits protein translation * side effects: photosensitivity
49
H1 receptor antagonist
* rapidly absorbed orally, widely distributed, rapidly metabolized via liver microsomes * treats: allergic reactions, motion sickness, nausea and vomiting in pregnancy, sleep aids * side effects: sedation, anti-muscarinic action, poisoning (esp. children) with convulsions, allergy, local anesthesia * **Diphenhydramine (Benadryl)** * **Tripelennamine (Pyribenzamine): OTC sleep aid** * **Meclizine (Dramamine II, Antivert), Hydroxyzine (Atarax): motion sickness** * **Promethazine (Phenergan): antiemetic** * **Chlorpheniramine (Chlor-Trimeton): component of cold medicine, less segating**
50
2nd generation H1 receptor antagonist
* treat allergic rhinitis; no sedation * poorly cross BBB so fewer side effects * **Loratadine (Claritin):** cardiovascular effects (rare with high doses) * **Fexofenadine (Allegra):** cardiovascular effects (rare with high doses) * **Azelastine (Astelin):** intranasal spray and opthlamic solution * **Cetirizine (Zyrtec)**
51
H2 receptor antagonists
* block gastric acid secretion (more so with nocturnal acid secretion than meal secretion) * treats dyspepsia, duodenal and gastric ulcers, hypersecretory conditions * CNS dysfunction possible * **Cimetidine (Tagamet):** antiandrogen (impotence and gynecomastia); inhibition of P450; most side effects of the H2 blockers * **Ranitidine (Zantac):** liver toxicity * **Famotidine (Pepcid)** * **Nizatidine (Axid):** least side effects of the H2 blockers
52
Cyproheptadine (Periactin)
* antihistaminic and antiserotinergic * treats skin allergies (urticaria, anti-5HT1), diarrhea of carcinoid syndrome (anti-5HT2) * side effects: sedation, antimuscarinic
53
ketanserin
* selective 5HT2A,2C receptor antagonist; α1 and H1 receptor antagonist * not used in US * **treats HTN** (relaxes vascular and tracheal smooth muscle), **antiplatelet aggregation**
54
Odansetron (Zofran) Granisetron (Kytril)
* 5HT3 receptor antagonist * **treats N/V in chemotherapy (v. effective)**
55
ergot alkaloids
* Agonist and antagonist actions at 5HT and α-adrenergic receptors * side effects: powerful hallucinations, smooth muscle contraction (vascular and uterine)
56
Ergotamine (Ergomar)
* ergot alkaloid; nonspecific partial agonist at all 5HT1,2 receptors; **partial agonist at α-adrenergic receptors** * Prevents migraines when taking during prodrome * side effects: N/V, cumulative and prolonged vasoconstriction
57
Methysergide (Cycloset)
* ergot alkaloid, partial agonist at all 5HT1 receptors, antagonist at 5HT2 * no longer on US market * migraine prophylaxis * side effects: GI disturbances, inflammatory fibrosis (chronic use), hallucinations
58
ergonovine
* ergot alkaloid; α-adrenergic receptor agonist * treats **postpartum hemorrhage (oxytocic)**
59
Bromocriptine (Sansert)
* ergot alkoloid; dopamine agonist * treats hyperprolactinemia
60
triptans
* non-ergot erotinin analogs; 5HT1B, D receptor agonists * **70% effective migraine treatment**
61
Acetylsalicylic acid (ASA, Aspirin)
* salicylate; **acetyl-salicylic acid irreversibly acetylates COX-1 and -2; metabolite (salicylic acid) reversibly inhibits COX-1 and -2** * at low doses ("baby aspirin") it irreversibly inhibits platelets, preventing thromboxane A2 formation * antiplatelet, analgesic and antipyretic, and anti-inflammatory (in ascending order of amount taken) * often taken as a "baby aspirin" to prevent MI, CVA * side effects: GI irritation, bleeding and anemia, hepatotoxicity, and salicylate toxicity * Nephrotoxicity in elderly or hypovolemic patients; rare HSRx
62
Diflunisal (Dolobid)
* salicylate; difluorophenyl derivitive of salicylic acid **reversibly inhibits COX-1 and -2** * treats osteoarthritis, strains/sprains, dental pain, and postepisiotomy pain * Fewer GI side effects and less effect on platelets than aspirin
63
Acetaminophen (Tylenol)
* Para-amino phenol; **reversibly inhibits COX1, 2 (favors COX-1)** * analgesic and antipyretic effect similar to aspirin, but weak anti-inflammatory effects * side effects: renal tubular necrosis if chronically abused with other NSAIDs; hepatic necrosis with overdose * **less GI irritation than aspirin** * Poor function in presence of peroxides (found in sites of inflammation); mostly metabolized via conjugation, but minor pathway via P450 enzymes may lead to toxic intermediate (N-acetyl-benzoquinoneimine)
64
Indomethacin (Indocin) Sulindac (Clinoril)
* indole; **reversible COX-1 and -2 inhibitor (favors COX-1)** * treats RA (10x as potent as aspirin), ankylosing spondyitis, osteoarthritis, gout * side effects: thrombocytopenia, asplastic anmia, severe frontal headaches * nephrotoxicity in elderly or hypovolemic patients * **sulindac:** half as potent as indomethacin; side effects less frequent
65
Ibuprofen (Advil, Motrin) Flurbiprofen (Ocufen) Naproxen (Aleve) Oxaprozin (Daypro)
* proprionic acid dervitive; **reversibly inhibits COX-1, 2 (favors COX-1)** * treats rheumatic disorders, osteoarthritis, ankylosing spondylitis, postpartum pain, dysmenorrheal pain * side effects: GI irritation; hepatotoxicity (less frequent than aspirin) * **naproxen:** longer half life than most proprionic acid derivatives (13 hrs vs. 1-2 hrs) * **oxaprozin:** 50 hr half life
66
Piroxicam (Feldene)
* enolic acid; reversibly inhibits COX-1, 2 (favors COX-1) * **Long-term treatment of RA** or osteoarthritis; also, ankylosing spondylitis, **acute musculoskeletal disorders,** acute gout * 45 hr half life allows for daily dosing; slow onset of action * same side effects as aspirin
67
Ketorolac (Toradol) Diclofenac (Voltaren)
* Heteroaryl acetic acid; **Reversibly inhibits COX-1, 2 (favors COX-1)** * **ketorolac:** use as alternative to opiods; post op pain, inflammatory eye conditions; injectable * **diclofenac:** long term treatment of RA or osteoarthritis; also, ankylosing spondylitis, migraines; can cause GI irritation
68
Celocoxib (Celebrex) Etoricoxib (Arcoxia)
* COX-2 inhibitor (selectively inhibits COX-2 because it is too bulky to reliably interact in COX-1 site) * has same anti-inflammatory, antipyretic, and analgesic effects as NSAIDs * less GI toxicity than traditional NSAIDs * contraindicated in patients with heart problems/pregnancy
69
Unfractionated heparin
* **Indirect thrombin inhibitor**; binds antithrombin potentiating formation of antithrombin-coagulation factor complex **(Xa, IIa)** * prevents/treats venous thromboembolism; maintains patency; **v. effective in cancer patients** * side effects: HIT **(binds PF4 which is highly immunogenic→activated platelets)**, bleeding; osteoporosis * given parenterally; monitored via PTT (want 2-2.5X normal value); **reversed by protamine**
70
Dalte**parin** (Fragmin) Enoxa**parin** (Lovenox) Fonda**parin**ux (Arixtra)
* indirect thrombin inhibitor; **LMWH that inhibits thrombin less effectively than Xa** * side effects: HIT, bleeding; osteoporosis and thombocytoenia * **dalteparin:** prevent thrombosis and embolism from clots * monitored by heparin assay (anti-factor Xa); longer half-life than heparin (1-2/day); **reversed by protamine** * **enoxaparin: drug of choice in pregnancy;** prevention/treatment of venous thromboembolism * monitored by heparin assay (anti-factor Xa); longer half-life than heparin (1-2/day); **reversed by protamine** * **​fondaparinux:** synthetic polysaccharide that binds active site of antithrombin (inhibits Xa); **given for HIT; no antidote**
71
Warfarin (Coumadin)
* **vit. K antagonist**; blocks vit. K-dependent gamma-carboxylation of factors **II, VII, IX, X, Protein C and S** (does not affect already synthesized factors) * used for **long term anticoagulation; valvular disease** * side effects: **thombosis (protein C depression),** bleeding; small therapeutic window; **teratogenic** * metabolism enhanced by drugs that induce P450 activity (e.g., barbiturates) * monitored by PT/INR; reversed by vit. K and factor concentrates
72
Bivalirudin (Angiomax) Argatroban (Acova)
* **direct thrombin inhibitor; inactivates fibrinogen-bound and unbound thrombin** * irreversible; no antidote * used as percutaneous coronary intervention * side effects: bleeding * Administered parenterally; monitored by PTT
73
Dabigatran (Pradaxa)
* **direct thrombin inhibitor**; inactivates fibrinogen-bound and unbound thrombin; **competitive inhibitor (reversible)** * treats DVT, PE, Afib * side effects: bleeding * Oral; renal fixed dose clearance (no monitoring); idarucizumab = antidote
74
Rivaro**xaban** (Xarelto) Api**xaban** (Eliquis)
* **direct Xa inhibitor;** reversibly bind active site of Xa * DVT/PE prophylaxis * side effeects: bleeding * oral; renal fixed dose clearance (no monitoring; andexanet = antidote
75
Al**teplase** Re**teplase** (Retavase) Tenec**teplase** (TNKase)
* fibrinolytic; **lyse already formed clots by activating plasminogen** * treats STEMIs * **alteplase:** acute stroke, PE * **reteplase:** less clot specific, more systemic activation * **tenecteplase:** more clot specific, less systemic activation
76
Clopido**grel** (Plavix) Prasu**grel** (Effient) Tica**grel**or (Brilinta)
* **antiplatelet; inhibits platelet ADP receptors** * prevent/treat ACS, stroke, peripheral vascular disease, agina; use s/p stent placement * side effects: bleeding (TTP rare) * **reversed by platelet transfusion**
77
Abciximab (Reopro)
* **antiplatelet; monoclonal antibody against GP IIb/IIIa** * side effects: may elicit immune response
78
Epti**fiba**tide (Integrilin) Tiro**fiba**n (Aggrastat)
* antiplatelet; **fibrinogen analog which competes with endogenous fibrinogen and vWF for IIb/IIIa** * side effects: bleeding; ACS; PCI; thrombocytopenia
79
Hydrocortisone
* steroid * treats dermatitis, psoriasis * side effects: **atrophy/thinning of skin (collagen),** stretch marks, talangiectasias, acne, cataract or glaucoma if applied near eye * **Systemical use affects hypothalamic-pituitary-adrenal axis→ growth retardation** * Seven classes (class I is strongest, class VII is weakest)
80
cyclosporine
* immunosuppressant * treats inflammatory conditions (e.g. psoriasis) * side effects: raises blood pressure→ kidney damage if used long-term
81
Methotrexate
* **folate analog; inhibits DHFR** * treats inflammatory conditions (psoriasis) and conditions needing immunosuppression * **hepatotoxicity** (develops slowly, can give up to 4.5 g over life); **pulmonary toxicity** (develops quickly); leukopenia; rarely, renal toxicity * **drugs increasing unbound protein (sulfa, salicylates, TCN, phenytoin) may cause methotrexate toxicity**
82
biologics
* block TNF-a * treats inflammatory conditions, arthritis * side effects: few (may unmask neurologic disease, latent infections (must do PPDs), malignancies) * $$$
83
UV light therapy
* **UVA, UVB, UVC; immunosuppression of T-cells via type I or type II reactions →** mono- or bifunctional adducts in DNA * treats inflammatory conditions (atopic dermatitis, CTCL, lichen planus, psoriasis) * side effects: skin cancer, thinning/leathering of skin * used with **psoralens (photosensitizing agents);** phenothiazines, thiazides, sulfonamides, NSAIDs, tetracycline, benzodiazapenes also sensitize skin
84
Isot**retin**oin (Accutane) Acit**retin** (Soriatane)
* **Retinoid; stimulates epithelial cell turnover; also anti-inflammatory** * good as adjunct to other therapies * **teratogenic effects** * **isotretinoin: acne**; teratogenic effects washes out in 3 wks * **acitretin: psoriasis;** teratogenic effects stays in fat stores for three years
85
​Primaquine (Primaryl)
* also a quinolone derivative but forms quinolone-quinone intermediates that oxidize schizont membranes **(only drug that inhibits exoerythrocytic schyzogony; kills at liver stage)** * **prevents relapses** * side effects: hemolysis (G6PD), methemoglobinemia, N/V/fever

GER MS2 Unit 2 (3 decks)

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