Pharmacology Flashcards
acetaminophen
扑热息痛,对乙酰氨基酚 reversibly inhibits COX, mostly in CNS (inactivated in peripheral) clinical use: antipyretic (扑热）， analgestic （熄痛）， NOT anti-inflammatory! used instead of Aspirin to avoid Reye’s syn in children with viral infection toxicity: 肝毒性（deplete glutathione in liver) antitode: N-acetylcystine (to regenerate glutathione)
Atropine
competitive antagonist at M2 (post-junctional muscarinic receptor in the heart) increase HR by blocking vagal firing
ALL (acute lymphoblastic leukemia) drugs: activated by? inhibited by?
6-mercaptopurine, 6-thioguanine purine analogs to inhibit de novo purine synthesis activated by HGPRT (hypoxanthine-guanine phosphoribosyl transferase) degraded by XO (xanthine oxidase) and thiopurine methyltransferase (TPMT) in the liver
Antidepressents的分类？机制？各自代表药物？
- ↑ 【NE] in the synapse: 1) ↑ its release (Bupropion） 2）↓ its re-uptake (SNRIs, TCAs) 3) inhibit metabolism (MAOI) 4) 去抑制：mirtazapine 2. ↑ 【5-HT] in the synapse: 1) ↑ its release (Bupropion） 2）↓ its re-uptake (SSRIs, SSNIs, TCAs, trazodone 三唑酮) 3) inhibit metabolism (MAOI)
atypical antipsychotics包括哪些？
“It’s atypical for Old Closets to Quietly riser from A to Z” Olanzapine 奥兰氮平 (significant weigt gain) Clozapine: 氯氮平 1. agranulocytosis - requires weekly WBC monitoring!!! (must watch clozapine closely!!!) 2. seizure 3.significant weigt gain Quetiapine 喹硫平 risperidone: ↑ prolactin (lactation + gynecomastia) ⟹ ↓ GnRH, LH, FSH ziprasidone 齐拉西酮 prolong QT interval
Benzodiazepines: 机制？用途？side effects? tolerance和什么相关? 分类？
机制: bind and enhance the inhibitory effects of GABAa 用途: 1. hypnotics 2. anxiolytics (for panic attacks, anxiety disorders) 3. anticonvulsants (seizures with alcohol withdrawal) 4. general anesthesia side effects: daytime drowsiness tolerance： the shorter the duration of action of a drug, the more likely withdrawal sym occur 分类
Benzodiazepines有2种用于epilepsy: which 2? for what kind of epilepsy? clinical use？ mechanism? side effects? notes?
diazepam, 地西泮; 安定 lorazepam 劳拉西泮 for what kind of epilepsy: status (DOC: lorazepam) mechanism: ↑ GABAa action side effects: sedation, tolerance, dependence, respiratory depression notes: also for for eclampsia seizure (子痫; DOC: MgSO4)
Bethanechol: 什么药？用途？ 同种药物还有哪些？
氨基甲酰甲基胆硷(胆硷能药) “Bethany, call me if you want to activate your bowel and bladder” - work on SMCs in the intestine and bladder; used to treat o.p. ileus, neurogenic ileus, urinary retention
benztropine
苯甲托品,苄托品 muscarinic antagonist, treat PD (Park my Benz)
bretylium
溴苄胺 inhibit NE release
Bupropion
antidepresant, has no side effect on sexual performance (while sexual dysfunction is seen in 50% patients treated with SSRIs) side effects: agitation, insomnia,
Buspirone
抗焦虑药， “I am always anxious if the “bus” will be “on time” with minimal to no hypnotic, sedative or euphoria effects; selective 5-HT1A R; safe and effective
carbachol
卡巴胆碱, 拟胆碱药 在青光眼和缩瞳中使用，降低球内压
buspirone: 什么药？机制？
抗焦虑
celecoxib
考塞来西，抗关节炎药 COX2 specific inhibitor spare COX-1, which helps maintain the gastric lining (NSAIDs and Aspirin: inhibits both COX1/2, decrease PG , which protects gastric lining) spares platelet function
cholinesterase inhibitor poisoning : syn, antidote?
Sym: DUMBBELSS (diarrhea , Urination Miosis, bronchospasm , bradycardia , lacrimation , sweating, salivation) Antidote : atropine + pralidoxime (解磷定Regenerate active AchE)
CNS stimulants: 包括哪些？机制？用途？
MMDP ↑ Catecholamines at synapes ADHD, narcolepsy, appetite control
clomiphene 同类药物还包括？ Mx Use Toxicity
SERMs
diaphoresis
发汗
Dimercaprol
二硫基丙醇 chelator of arsenic, treat arsenic posioning
Diphenhydramine: 什么药？机制？ 副作用？
苯海拉明， 1st generation anti-histamine (H-1 blocker) anti-allgery drug, 第一代抗组胺药（Diphenhydramine， chlorphe’niramine 扑尔敏)副作用很多： 1) anti-muscarinic (pupillary dilation, dry mouth, urinary retention, constipation) 2) anti- alpha adrengenic 3) anti-serotonergic
DOC for absence seizure?
1st line: ethosuximide 2nd line: valproate
DOC for complex partial?
carbamazepine
DOC for eclampsia seizure?
子痫 DOC: MgSO4 can also use benzodiazepines (diazepam, lorazepam)
DOC for myoclonic seizures?
Valproic acid (sodium valprote)
DOC for myoclonic?
valproic acid
DOC for simple seizures?
carbamazepine
DOC of trigeminal neuralgia? mechanism? toxicity? 对P450影响？
carbamazepine inhibit Na+ channel toxicity: aplastic aneima, agranulocytosis (have to check CBC regularly) P450 inducer to ↑ metabolism of many drugs, so ↓ the drugs’ effectiveness
DOC for tonic-clonic?
phenytoin, carbamazepine, valproate
donepezil
多奈哌齐 (益智药） anticholinesterase, 增强胆碱能药物，treat AD
drug choice for HTN and BPH (benign prostatic hyperplasia)?
“osin” a1 blockers: relax VSMCs in arteries, also relax muscles around bladder neck and prostate
edrophonium
腾喜龙 [氯化腾喜龙试验诊断重症肌无力] Cholineasterase inhibitors
Epinephrin: receptor?
a1, a2, b1, b2 a1: constrict VSMCs in skin and viseral - increase BP b1: in heart, increase HR b2: dilate VSMCs in skeletal muscles - decrease diastolic BP (和a1作用正相反） Epi at low dose: b2 > a1 - decrease in diastolic BP Epi at high dose: a1 > b2 - increase in both systolic and diatolic BP
eplerenone: what drug is this? side effect?
newer generation of aldosterone inhibitor, most common side effect: gynecomastia (男子女性型乳房）
metyrosine
甲基酪氨酸，美替罗星 (降压药） 抑制tyrosine代谢为DOPA
flunisolide
氟尼缩松，9-去氟肤轻松 for asthma
flunisolide
9-去氟肤轻松[糖皮质激素] 用于inhalar for persistent bronchial asthema
Fluoxetine [flu:’oksetine]
氟西汀,百忧解 serotonin reuptake inhibitor, elongate the effect of serotonin, treat depression
Scopolamine [skou’polemin]
东莨菪碱; 天仙子碱 selective muscarinic R antagonist 治疗MG药物， pyridostigmine对GI的副作用
Furosemide
“速尿“ loop diuretics,作用在亨利管 利尿mechanisms: 1) inhibit Na/K-2CL co-transporter in the ascending limp of the loop of Henle 2) stimulate PG release for vasodilation
treatment for MG (myasthenia gravis)
- cholinesterase inhibitor (pyridostigmine 吡斯的明，美定隆）: has GI side-effect by stimulating the gut muscarinic cholinergic R. 胃肠道副作用用Scopolamine (selective muscarinic R antagonist)治疗， which won’t affect the act of pyridostigmine on nicotinic cholinergic R in muscle Note: 和Pilocarpine对比：pilocarpine is a non-selective muscarinic R antagonist, which will worsen the MG sym 2. immunosuppresent 3. thymectomy
gemfibrozil
吉非贝齐, 调血脂药, 用于降TG one of the “fibrates”, to increase the cholesterol content of bile, can precipitate for gallstone formation similar risk for gallstone formation as the bile acid-binding resins (cholestyramine, colestipol, colesevelam)
guanethidine
胍乙啶（一种降血压药） inhibit NE release
haloperidol
氟派啶醇 抗精神病药 commonly used in agitation; the drug most commonly associated with NMS (neuroleptic malignant syn) 过度抑制dopamingergic （尤其是D2 receptor)引起 NMS4大特征：高温（dopaminergic系统调控体温，muscle tone/movement), 全身僵硬，autonomic instability, altered mental status 无法预防NMS， 出现症状后用bromocriptine （dopamine agonist) or dantrolene （肌松剂）治疗
haloperidol
氟派啶醇 commonly used in agitation; the drug most commonly associated with NMS (neuroleptic malignant syn) 过度抑制dopamingergic （尤其是D2 receptor)引起 NMS4大特征：高温（dopaminergic系统调控体温，muscle tone/movement), 全身僵硬，autonomic instability, altered mental status
If a pt with history of seizure and mental illness presents with gingival hyperplasia, which drug causes it? Mechanism of this drug? Use? toxicity?
Phenytoin Mechanism: inhibit Na+ channel Use: for partial seizures, tonic-clonic (grand mal) seizures, and status epilepticus toxicity: 1. very narrow therapeutic window 2. major CNS sym: ataxia + nystagmus 3. megablostic anemia 4. ↑ P450 activity, to decrease the blood level of many drugs (因为加快了其代谢） 5. 如果用于孕妇，fetal hydantoin syn 胎儿乙内酰脲综合征
ipratropium
异丙托铵(支气管扩张药) muscarinic antagonist, 作用于呼吸系统。胆碱能系统激活时，支气管痉挛，所以拮抗剂会使气道扩张。 Dx: COPD, asthma
isoproterenol
activate b1 and b2 - increase HR and decrease BP (dilate vessels)
Lithium: 用途？副作用？
用途： mood stabilizer for bipolar; also SIADH side effects: “LMNOP”
lorazepam clinical use？ mechanism? side effects? notes?
劳拉西泮,氯羟安定 DOC in status epilepticus （持续性癫痫） mechanism: ↑ GABAa action side effects: sedation, tolerance, dependence, respiratory depression notes: also for for eclampsia seizure (子痫; DOC: MgSO4)
MAO
monoamino oxidase, degrade NE, DA and serotinin MAO inhibitors are used for depression
MAOI: 包括哪些药（口诀）？ 机制？ Rx? toxicity? contradiction?
“MAO Takes Pride In Shanghai” Tranylcypromine: 反苯环丙胺 ‘phenelzine Isocarboxazid 异卡波肼 selegiline: 司来吉兰 (selective for MAO-B) 机制: non-selective inhibition of MAO - ↑ amine neurotransmitters (NE, 5-HT, DA) Rx: 1) atypical depression 2) anxiety 3) hypochondriasis 疑病[症] toxicity: 1) hypertensive crisis (if digest tyramine from wine and cheese) 2) CNS stimulation contradiction: SSRIs, TCAs, meperidine (哌替啶; 度冷丁), and dextramethorphan 右甲吗南, (鸦片类镇咳药)
mestranol [`mestrənɔl] 同类药物还包括？ Mx Use Toxicity
美雌醇，为口服激素避孕药中的雌激素成分
methacholine
muscarinic chonlinergic agonist induce bronchial SMC contraction - induce asthma mechacholine challenge test: Dx for asthma
drug selection for isolated HTN? for HTN + DM? list side effects: 1. doxazosin 2. propranolol 3. ramipril 4. hydrochlorothiazide 5. elephenone 6. verapamil 7. amlodipine 8. isosorbide dinitrate
for isolated HTN: thiazide diuretics + DHP CCB (dihydropyridine CCB, such as Amlodipine) for HTN + DM: ACE I or ARB side effects: 1. a1 selective blocker: 1st dose hypotension 2. non-selective b blocker: asthma, bradycardia, worsen peripheral vascular disease 3. ACE I: angioedema (swollen of lips, 舌, - 与peripheral edema 如flushing + ankle swelling区别）， cough, 1st-dose hypotension 4. 1st line anti-HTN drug? 5. aldosterone inhibitor: gynecomastia 男性乳房女性型化 6. CCB more selective to heart: constipation, gingival hyperplasia 7. CCB selective for vessels: flushing, peripheral edema 8. nitrates: headache, contraindicated for drugs for ED (the PDE inhibitors “fil”s
methotrexate
甲氨喋呤 (MTX), DOC for early (< 6wks gestational age) ectopic pregnancies irreversibly inhibits DHF reductase
Prazosin
哌唑嗪,降压新 alpha-1 adrenergic antaognist
mirtazapine
米尔塔扎平(抗抑郁症) de-inhibit the a2 R
finasteride [fi’nasteride]
非那司提(治疗良性前列腺增生) 5 a-reductase inhibitor 同类药有dutasteride
niacin: use, side effect and drug interacitons
used to decrease LDL side effect: when niacin is initiated, most patients experience warmth, flushing, itchiness of the skin - caused by prostaglandins - can be relieved by giving aspirin 30 min before administration interact with anti-HTN drugs: niacin is a vasodilator interact with anti-DM drugs: increase insulin resistance
niacin: use, side effect and drug interacitons
used to decrease LDL side effect: when niacin is initiated, most patients experience warmth, flushing, itchiness of the skin - caused by prostaglandins - can be relieved by giving aspirin 30 min before administration interact with anti-HTN drugs: niacin is a vasodilator interact with anti-DM drugs: increase insulin resistance can increase uric acid - watch out for gout patient!
nitroprusside: use, toxicity, antitode
硝普盐，rapid-onset visodilator (within 30 sec), used in emergency to control BP; metabolized to NO and cyanide； cyanide metabolized by the liver (adding a sulfur) to form thiocyanate; major risk is cyanide toxicity; give sulfur to enhance conversion of cyanide to thiocynate
NMS: Cx? Rx?
neuroleptic malignant syndrome: 抗精神病药的恶性综合征:一种罕见的有时是致死的反应,特点为高烧、强直及昏迷 Cx: “FEVER”: Fever, Encephalopathy Vitals unstable Enzyme ↑ (myoglobinuria) Rigidity of muscles Rx: dantrolene 肌松药 + D2 agonists (bromocriptine)
NSAID
diclofenac: 双氯芬酸, 双氯灭痛 indomethacin : 吲哚美辛. 消炎痛 piroxicam: 吡罗昔康,吡氧噻嗪,炎痛喜康 reversibly inhibit COX1 and COX2
Reserpine
利血平 利舍平对NE神经末梢中的囊泡膜具有很高的亲和力，能与囊泡膜上胺泵（依赖于Mg2+-ATP的胺类主动转运机制）呈难逆性结合，使囊泡膜失去摄取和贮存去甲肾上腺素和多巴胺的能力，从而使囊泡内递质的合成与贮存逐渐减少，以至耗竭，使去甲肾上腺素能神经冲动传递受阻，从而产生降压作用并伴有心率减慢。
pen’tazocine: 什么药？ Mechanism? side effect?
喷他佐辛; 镇痛新 opioid narcotic with partial agonist activity + weak antagonist activity at mu receptor; 能有效镇痛，但是很少abuse potential side effect: cause withdrawal sym in pts who are dependent or tolerant to morphine or other opioids
phenoxybenzamine
苯氧苯扎明, 苯氧苄胺(降压药) non-selective alpha-adrenergic antagonist, treat pheochromocytoma
Phentolamine
non-selective a1, a2 blockers
Phenylephrine
selective a-agonist, stimulate both a1, a2
Phenytoin: when used for epilepsy, for what kind?？ mechanism? kinetics? side effects? notes?
when used for epilepsy, for what kind： all partial (simple, complex) and tonic-clonic [1st line], status epilepticus [1st line + DOC for prophylaxis] mechanism: ↑ Na+ channel inactivation; kinetics: zero order side effects: ↑ P450, Stevens-Johnson syn [(SJS) is a milder form of toxic epidermal necrolysis (TEN)], SLE-like syn, teratogenesis, notes: Fosphenytoin for parenteral use
polyethylene glycol
聚乙二醇, osmotic laxative
G-protein class with receptors for sympathetic, para, etc： 记忆口诀？
QISS (kiss) and QIQ (kik) till you are SIQ (sick) of sqs (super kincky sex) QISS = sympathetic Receptors α1, α2,β1, β2 QIQ = parasympathetic Receptors M1, M2, M3 SIQ SQS = dopamine D1, D2, Histamine H1, H2, vasopressin V1, V2
downstream signaling for Gq?
R → PLC → lipids converted into PIP2 → DAG / PKC, and IP3 (【Ca2+]in
Rx: ADHD?
methylphenidate 哌醋甲酯,利地林
Rx: alcohol withdrawal
BZDs
Rx: anxiety
- SSRIs (-etine, ie: flurexine; pa’roxetine, sertraline, citalopram: “flashback paralyzed senior citizens” 2. SNRIs (Venlafaxine 文拉法辛, duloxetine 度洛西汀) 3. busprione
Rx: bipolar
- Mood stabilizers: Lithium, Valproic acid carbamazepine 2. atypical antipsychotics
Rx: bulimia
神经性贪食症 SSRIs (flurexine; pa’roxetine, sertraline, citalopram: “flashback paralyzed senior citizens”)
Rx: depression 如果合并失眠用什么药？
- SSRIs 2. SNRIs 3. TCAs 4. bupropion 5. mirtazapine 米尔塔扎平(抗抑郁症) - used when depression + insomnia
Rx: OCD?
obsessive-compulsive disorder SSRIs clomipramine 氯丙咪嗪,海地芬[抗抑郁药, 一种TCA] TCA ends with -ipramine or -iptyline
Rx: Panic disorder
- SSRIs 2. venlafaxine (文拉法辛, 一种SNRI) 3. BZDs
Rx: PTSD
SSRIs (flurexine; pa’roxetine, sertraline, citalopram: “flashback paralyzed senior citizens”) most effective is therapy!
Rx: social phobias?
- SSRIs (flurexine; pa’roxetine, sertraline, citalopram: “flashback paralyzed senior citizens”) 2. b-blockers
Rx: Tourette syn
antipsychotics (haloperidol, risperidone)
side effect and drug interaction of niacin?
gout facial flushing and warmth (can be prevented by aspirin, mediated by prostagladin) can dilate arteries - if combined with anti-HTN drug, have to lower the dose can increase insulin resistance - if combined with anti-DM drugs, have to increase the dose
side effect of niacin?
gout facial flushing and warmth (can be prevented by aspirin, mediated by prostagladin)
side effects of statins?
myopathy; hepatitis
SSRIs: (specific serotonin reuptake inhibitors) “Flashbacks Paralyze Senior Citizens”
flu’oxetine： 氟西汀,百忧解 pa’roxetine: ,帕罗西丁 ‘sertraline: 舍曲林 citalopram: 西酞普兰
summary of side effects of chemo drugs
vincristine: 外周神经毒性 neurotoxicity (interfere with microtubule formation in the nerve axons)- finger numbness and tangling cyclophosphamide : 出血性膀胱炎 burning on urination and urgency (cyclophosphamide- or ifosfamide-induced hemorrhagic cystitis) cisplatin： 肾毒性 （生成ROS, 损伤肾小管）， 预防需要1）IV 大剂量生理盐水； 2）amifostine: thiol-based free-radical scavenger methotrexate (MTX) overdose: leucovorin (folinic acid) to treat vomit and nausea: 5-HT3 receptor antagonists (-setrons, such as ondansetron, granisetron, dolasetron) “tumor lysis syn”: 电解质紊乱+急性肾衰， 解毒用aggressive hydration + alkalinization of the urine + allopurinol (别嘌呤醇) Mesna: prevent hemorrhagic cystitis in patients receiving cyclophosphamide or ifosfamide; Mesna binds acrolein, the toxic metabolite formed by these agents.
Tardive dyskinesia: 什么药物的副作用？
抗精神病药
TCA: 词尾？以及2个特例？ 机制？ Rx? toxicity?
词尾: - ipramine (imipramine, desipramine, clomipramine) - iptyline (amitriptyline, - 3°TCA; nortriptyline -2°TCA) 2个特例: ‘doxepin 多虑平; amoxapine 阿莫沙平 机制: inhibit both NE and 5-HT re-uptake Rx: 1) major depression 2) OCD (clomipramine 氯丙咪嗪) 3) fibromyalgia 纤维肌痛 toxicity: TCA = Tir-C’s (convulsion, coma, cardiotoxicity)
terbinafine
特比萘芬, 疗霉舒
trazodone
曲唑酮,三唑酮 inhibit 5-HT re-uptake: anti-depressent
O’meprazole
奥美拉唑 proton pump inhibitor, inhibit the H/K ATPase → ↓ of [HCL] in the gastric lumen
typical antipsychotics: 包括哪些？其中哪些high potency? 哪些low potency?-各自副作用？ 机制？用途？ 药代动力学特点？ toxicity? 最特别和致命的toxicity?
包括哪些： haloperidol + “-azines” high potency: “Try to Fly High” (trifluoperazine, fluphenazine, haloperidol) - neurological side effects low potency: “Cheating Thieves are low) (chlorpromazine 氯丙嗪, thioridazine 硫利达嗪; 机制: block D2 receptor, ↑ [cAMP] 用途: schizophrenia, psychosis, acute mania, Tourette syn 药代动力学特点： high lipid soluble, very slow to clear Toxicity: 1. extrapyramidal system (EPS): dyskinesia 2. endocrine (DA antagonism): hyperprolactinemia, 这些病人常有泌乳；galactorrhea 3. anti muscarinic (dry mouth, constipation) 4. anti-alpha 1 (hypotension) 5. anti-histamine: sedation 最特别和致命的toxicity: NMS, tardive dyskinesia
Venlafaxine 什么药？用途？toxicity?
文拉法辛 SNRI，inhibit both NE and 5-HT re-uptake 用途：1) depression 2) generalized anxiety disorder 3) panic disorder toxicity: increase BP
wafarin drug interaction
enhancers for cytochrome P-450 (therefore decrease efficacy of warfarin): rafampicin 利福平, phenobarbital, phenytoin [记忆法：RPP enhance my score】 inhibitors for cytochrome P-450 (therefore enhance efficacy of warfarin): amiodarone, cimentidine, TMP-SMX (trimethoprim-sulfamethoxazole)复方新诺明 【记忆法：ACT]
