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Pharmacology > Pharm 1 (autonomics, hematologics, antineoplastics) > Flashcards

Pharm 1 (autonomics, hematologics, antineoplastics) Flashcards

1
Q

Ephedrine

A

Indirect sympathomimetic - indirect general agonist, releases stored catecholamines

Nasal decongestion, urinary incontinence, hypotension

pseudoephedrine commonly used

*activity reduced by prior tx w/ reserpine/guanethidine

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2
Q

Amphetamine

A

Indirect sympathomimetic - indiret general agonist, reuptake inhibitor, & releases stored catecholamines

Tx - Narcolepsy, obesity, attention deficit disorder

*activity abolishied by prior tx w/ reserpine/guanethidine

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3
Q

Cocaine

A

Indirect symphathomimetic - indirect general agonist & reuptake inhibitor

Causes vasoconstricion & local anesthesia

NEVER give β-blockers if cocaine intoxication is suspected (can lead to unopposed α1 activation & extreme hypertension)

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4
Q

Prazosin
Terazosin
Doxazosin
Tamsulosin

A

α1 selective antagonist (-osin)

Urinary symptoms of BPH, HTN, PTSD (prazosin)

Tamsulosin - solely used for BPH (α1a selective)

AE - 1st dose orthostatic HoTN, dizziness, headache

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5
Q

Yohimbine

A

α2 antagonist - increases central sympathetic activity
= ↑ BP & HR

Tx - male erectile dysfunction, HoTN

AE - anxiety, (excess pressor effect if NET1 is blocked)

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6
Q

Phenoxybenzamine

A

Irreversible nonselective α antagonist (long DoA)
= ↓ BP, ↑ HR (baroreflex +)

Tx - pheochromocytoma (catecholamine releasing tumor in the adrenal gland)

AE - orthostatic HoTN, reflex tachycardia, MI

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7
Q

Phentolamine

A

Reversible nonselective α antagonist

Given to Pt on MAOI who eat tyramine-containing foods

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8
Q

Mirtazapine

A

α2 selective antagonist

Tx - Depression

AE - Sedation, ↑ serum cholesterol & appetite

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9
Q

Labetalol

Carvedilol

A

Nonselective α- & β-antagonists
=↓ BP w/ limited HR ↑ (↓ reflex tach by also blocking α1)

Tx - HTN

(-ilol & -alol instead of -olol of B selective)

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10
Q

Nadolol
Pindolol
Propranolol
Timolol

A

Nonselective β-antagonists (β1=β2)
= ↓ HR, BP & reduce Renin

Tx - HTN, angina pectoris, arrhytmias, migraine, hyperthyroidism

↑ bronchospasm (β2)

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11
Q 
Atenolol
Metoprolol
Esmolol
Beliprolol
Acebutolol
A

Selective β-antagonists (β1>β2)
= ↓HR, BP & reduce renin
safer on asthma

Tx - HTN, angina pectoris, arrhytmias

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12
Q

Pindolol & Acebutolol

A

β-antagonists w/ ISA (intrinsic sympathomimetic activity)
=↓BP, but only modestly ↓ HR
block receptors but elicit a small response

Tx - HTN, arrhytmias, migraine

may avoid worsening of bradycardia

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13
Q

β-blockers

A

-olol (-alol, -ilol)

Tx - angina pectoris (↓HR & contractility = ↓ O2 need)

  • MI (↓ mortality - metoprolol, carvedilol, bisoprolol)
  • SVT (↓ AV conduction, class II - metoprolol esmolol)
  • HTN (↓ CO, ↓ renin (due to blockade of JGA cells)
  • CHF (slows progression of chronic failure)
  • Glaucoma (↓ secretion of aqueous humor - timolol)

AE - impotence, CV (bradycardia, AV block, CHF), dyslipidemia (metoprolol), CNS (seizures, sedation)

may cause exaceration in asthma/COPD (especially nonselective, through blockade of β2)

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14
Q

Phenylephrine

A

Direct sympathomimetics - α1>α2 (=vasoconstriction)
= ↑ BP, ↑ TPR & reflex bradycardia

Tx - HoTN, ocular procedures (mydriatic), decongestant

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15
Q 
Albuterol
Salmeterol
Terbutaline
(Metaproterenol)
(Ritodrine)
A

Direct sympathomimetics - β2>β1 (=bronchorelaxation)

Tx - Acute asthma (albuterol)

 - Long-term asthma/COPD (Salmeterol)
 - Reduce premature uterine contractions (terbutaline)
     - ritodrine designed specifically as uterine relaxant
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16
Q

Isoproterenol

A

Direct sympathomimetic - β1=β2
= ↓ TPR, ↑ HR, ↑ myocardial contractility

Tx - Electrophysiologic evaluation of tachyarrhythmias
can worsen ischemia

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17
Q

Dobutamine

A

Direct Sympathomimetic - β1>β2,
= + inotropic, + chronotropic, (TPR not affected)

Tx - heart failure (inotropic>chronotropic), stress testing

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18
Q

Epinephrine

A

Direct sympathomimetic = β>α
(α effects dominate at high doses)

Tx - Anaphylaxis, open angle glaucoma, asthma, HoTN

CI - PT using nonselective β-blockers (=severe vasoconstriction)

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19
Q

Norepinephrine

A

Direct sympathomimetic = α1>α2>β1
↑ BP, PP, TPR & Coronary flow, ↓ CO & renal perfusion

Tx = HoTN (but ↓ renal perfusion) - dose titration needed

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20
Q

Dopamine

A

Direct sympathomimetic - D1=D2>β>α
(inotropic & chronotropic α effects predominate at high dose)

Unstable bradycardia, heart failure, shock

Hypovolemia should always be corrected before use
Avoid w/ MAOI or tricyclic antidepressants

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21
Q

Fenoldopam

A

Direct agonist - D1 selective

Tx - Hypertensive crisis (renal, mesenteric, peripheral & coronary vasodilation) (= renal blood flow maintained & natriuresis promoted)

AE - HoTN

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22
Q

Clonidine

α-methyldopa

A

Sympatholytics - α2 selective agonist
(↓ BP by ↓ central sympathetic outflow)

Tx - Hypertensive urgency (doesn’t ↓ renal blood flow)

α-methyldopa for HTN in pregnancy (safe in pregnancy but causes DIrect Coombs + hemolytic anemia, SLE-like syndrome)

Clonidine AE - CNS depression bradycardia, HoTN, respiratory depression & small pupil size

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23
Q

Atropine
Homatropine
Tropicamide

A

Muscarinic antagonists

Organ system - eye

Tx - produce mydriasis & cycloplegia

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24
Q

Ipratropium

tiotropium

A

Muscarinic Antagonists

Organ system - respiratory

Tx - COPD, asthma (↓ bronchoconstriction & bronchial secretions)

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25
Atropine
Muscarinic antagonist - used to treat bradycardia & for ophthalmic applications Blocks DUMBBeLSS ``` Eye - pupil dilation, cycloplegia airway- ↓ sectretions Stomach - ↓ acid secretion Gut - ↓ motility bladder - ↓ urgency in cystitis ``` AE - Hot, Dry, Red, Blind, Mad ↑ temp (by ↓ sweating); rapid pulse; dry mouth; dry, flushed skin; cycloplegia; constipation; disorientation Causes acute angle-closer glaucoma in elderly (due to mydriasis), urinary retention in men w/ prostatic hyperplasia, & hyperthermia in infants
26
Benztropine
Muscarinic antagonist Organ system - CNS Tx - Parkinson disease =re-establishes dopaminergic-cholinergic balance
27
Scopolamine
Muscarinic antagonist Organ system - CNS Tx - Motion sickness
28
Oxybutynin Darifenacin Solifenacin
muscarinic antagonist Organ system - Genitourinary Tx - Reduce urgency in mild cystitis & ↓ bladder spasms (Other agents - tolterodine, fesoterodine, trospium)
29
Hexamethonium | Mecamylamine
Nicotinic Antagonists ↓ predominant autonomic tone & prevent baroreflex SANS - arterioles = vasodialtion & HoTN - Veins = Dilation, ↓ venous return, ↓ CO - Sweat glands = Anhidrosis PANS - Heart = tachycardia - Iris = Mydriasis - Ciliary muscle = Cycloplegia (loss of accommodation) - GI = ↓ tone & motility = constipation - Bladder = urinary retention - Salivary glands = Xerostomia
30
Succinylcholine | d-Tubocurarine
Nicotinic Antagonists block Nm channel (neuromuscular blockade) S-bind & keep channel open=persistent depol & paralysis T-bind and prevent openeing of channel Tx of convulsions, & ↓ neuromuscular transmission during anesthesia; used in tracheal intubation to control ventilation
31
Methacholine
Cholinomimetic agent - Direct agonist = stimulates muscarinic receptors in airway when inhaled Tx - Challenge test for diagnosis of asthma
32
Carbachol
Cholinomimetic agent - Direct agonist = "CARBon copy" of AcetylCHOLamine Tx = Glaucoma, pupillary constriction, & relief of intraocular pressure *High doses may induce cardiac arrest*
33
Bethanechol
Cholinomimetic agent - Direct agonist = activates Bowel & Bladder smooth muscle cells - resistant to AChE Tx - Post-op ileus, neurogenic ileas, urinary retention
34
Muscarine Poisoning
Salivation, sweat, tear flow Abdominal pain, N, D Blurred vision, dyspnea severe = cardiac & respiratory failure Wet
35
Pilocarpine
Cholinomimetic agent - Direct acting = Contacts ciliary muscle of eye (open-angle), & pupillary sphincter (closed-angle) - Resistant to AChE Tx - Open & Closed-angle glaucoma - Potent stimulator of sweat, tears, & saliva (cry, drool, & sweat on your PILOw)
36
Edrophonium
Indirect acting cholinomimetic = anticholinesterase = ↑ endogenous ACh - Short acting Dx myasthenia gravis (historical; now dx w/ anti-ACh↑R A ↑ ACh makes better = MG; worse = cholinergic crisis
37
Neostigmine
Indirect acting cholinomimetic = anticholinesterase = ↑ endogenous ACh - intermediate acting No CNS penetration Tx - Post-op & neurogenic ileus & urinary retention; myasthenia gravis, reversal of Nm junction blockade (post-op)
38
Pyridostigmine
Indirect acting cholinomimetic = anticholinesterase = ↑ endogenous ACh; ↑ strength - long lasting Does not penetrate CNS Tx - Myasthenia gravis (pyRIDostiGMine)
39
Physostigmine
Indirect acting cholinomimetic = anticholinesterase = ↑ endogenous ACh crosses BBB = enters CNS Tx - anticholinergic toxicity (phyxes atropine overdose)
40
Donepezil Rivastigmine Galantamine (Tacrine)
Indirect acting cholinomimetic = anticholinesterase = ↑ endogenous ACh Lipid soluble - CNS entry Tx - Alzheimer disease
41
Anticholinesterase poisoning
often due to organophosphates, like parathion, that irreversibly inhibit AChE =DUMBBELSS Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Excitation (of skeletal muscle & cns), Lacrimation, Sweating, Salivation Antidote = atropine (competitive inhibitor) + pralidoxime (regenerates AChE if given early)
42
Heparin (Enoxaparin - LMWH) (Fondaparinux)
Indirect Xa inhibitor (cofactor for the activation of antithrombin) = ↓ thrombin & ↓ factor Xa Tx - Immediate anticoagulation for PE, acute coronary syndrome, MI, DVT - Used during pregnancy (doesn't cross placenta) Monitor w/ PTT Antidote = protamine sulfate AE - bleeding, HIT, osteoporosis, drug-drug interactions
43
Argatroban Bivalirudin (Lepirudin)
Direct thrombin inhibitors (derived of hirudin from leeches) Tx - anticoagulation in Pt w/ HIT
44
(Dabigatran)
Direct thrombin inhibitor - Oral Tx - stroke prevention in Pt w/ A. Fib - prevention of DVT & PE *shown to be as effective as warfarin w/ less bleeding/hemorrhage risk
45
Warfarin
Vitamin K antagonist = inhibits synthesis of II, VII, IX, X & Protein C, S Tx - Chronic anticoagulation (after STEMI, venous thromboembolism propylaxis, prevention of stroke in A. Fib) - crosses placent = NOT used in pregnancy Monitor w/ PT/INR (effects extrinsic pathway) Antidote = Vitamin K AE - Bleeding, teratogenic, skin/tissue necrosis, drug-drug interactions
46
Rivaroxaban | Apixaban
Direct Factor Xa inhibitors (bind & directly inhibit Xa) Tx - stroke prophylaxis in Pt w/ A. Fib - Tx & prophylaxis of DVT & PE (rivaroxaban) AE - Bleeding (no specific reversal agent)
47
Alteplase (tPA) Reteplase (rPA) Tenecteplase (TNK-tPA)
Thrombolytics = directly or indirctly aid conversion of plasminogen to plasmin = cleaves thrombin & fibrin clots = ↑PT, PTT (no change in platelet count) Tx - Early MI, early ischemic stroke, direct thrombolysis of severe PE AE - Bleeding CI - PT w/ active bleeding, Hx of intracranial bleeding, recent surgery, known bleeding diatheses, severe HTN Antidote = aminocaproic acid (inhibits fibrinolysis) -FFP or cryo can also be used to correct factor deficiency
48
Aspirin (ASA)
Antiplatelet drug = Irreversibly inhibits COX (1&2) enzyme by covalent acetylation -acts until new platelets produced ↑ bleeding time, ↓TXA & prostaglandin (no effect PT/PTT) Tx - antipyretic, analgesic, anti-inflammatory, antiplatelet (↓ aggregation) AE - Gastric ulceration, tinnitis (CN VIII) - Chronic use = acute renal failure, interstitial nephritis, & upper GI bleeding - Reye syndrome in children w/ viral infection Overdose = respiratory alkalosis then metabolic acidosis
49
Clopidogrel Prasugrel Ticlopidine Ticagrelor
Inhibit platelet aggregation by irreversibly blocking ADP receptors. (Inhibit fibrinogen binding by preventing glycoprotein IIb/IIIa from binding to fibrinogen) Tx - acute coronary syndrome; coronary stenting - ↓ incidence of recurrence of thrombotic stroke AE - TTP/HUS may be seen - Neutropenia (ticlopidine)
50
Dipyridamole | Cilostazol
Antiplatelet drug = Phosphodiesterase III inhibitor - ↑ cAMP in platelets = inhibit aggregation; (vasodilators) Tx - intermittent claudication, coronary vasodilation, prevention of stroke or TIAs (combo w/ aspirin), angina prophylaxis AE - N, H, facial flushing, HoTN, abdominal pain
51
Abciximab Eptifibatide Tirofiban
GP IIb/IIIa receptor antagonists = prevent aggregation Abciximab is made from monoclonal Ab Fab fragments Tx - Unstable angina, percutaneous transluminal coronary angioplasty (PCI) AE - Bleeding, Trhombocytopenia
52
(Vorapaxar)
PAR (protease activated receptor) antagonist = inhibits effects of thrombin on platelets Tx - ↓ thrombotic CV events in Pt w/ established PAD or history of MI AE - intracranial hemorrhage CI - Pt w/ active bleeding, history of intracranial bleed, or previous TIA/stroke
53
Methotrexate
Folic acid analog - inhibits dihydrofolate reductase = ↓ dTMP = ↓ DNA & protein synthesis Tx - leukemias, lymphomas, choriocarcinoma, sarcomas - abortion, ectopic pregnancy, RA, psoriasis, IBD AE - myelosuppression (reversible w/ leucovorin "rescue") Macrovesicular fatty change in liver, Mucositis, Teratogenic
54
5-Flourouracil (5-FU)
Pyrimidine analog bioactivated to 5F-dUMP, which covalently complexes folic acid = inhibits thymidylate synthase = ↓dTMP = ↓ DNA & protein synthesis Tx - Colon cancer, pancreatic cancer, - topical for basal cell carcinoma AE - Myelosuppression (NOT reversible w/ leucovorin), photosensitivity Overdose - "rescue" w/ uridine
55
Cytarabine | Fludarabine
Pyrimidine analog = inhibition of DNA polymerase Tx - Leukemias & lymphomas - ara-C = most important antimetabolite in AML tx AE - Leukopenia, thrombocytopenia, megaloblastic anemia (CYTarabine causes panCYTopenia) - high CNS levels = cerevellar syndrome (Dyarthria, nystagmus, ataxia)
56
Azathioprine 6-mercaptopurine (6-MP) 6-thioguanine (6-TG)
Purine analog = ↓ de novo purine synthesis; activated by HGPRT Tx - Leukemia - Preventing organ rejection, RA, SLE (A), IBD (6s) AE - Bone marrow suppression, GI & liver - Azathioprine & 6-MP are metabolized by xanthine oxidase = both ↑ toxicity w/ allopurinol, which inhibits their metabolism
57
Cyclophosphamide | Ifosfamide
Nitrogen mustard - covalently cross-link DNA at guanine N-7. Require bioactivation in the liver Tx - Solid tumors, leukemia, lymphomas & some brain cancers AE - Myelosuppression, *Hemorrhagic cystitis (partially prevented w/ mesna - binds toxic metabolites)
58
Carmustine Lomustine Semustine Streptozocin
Nitrosoureas - Cross-link DNA, cross BBB, require bioactivation Tx - Brain tumors (including glioblastoma multiforme) - wafers placed in brain cavity to kill potential microsatellite tumors after surgery AE - Profound myelosuppression, CNS toxicity (convulsions, dizziness, ataxia)
59
Busulfan
Cross-links DNA Tx - CML - used to ablate pt's BM before BM transplant AE - sever myelosuppression (in almost all cases), pulmonary fibrosis, hyperpigmentation
60
Cisplatin | Carboplatin
Platinum compounds = Cross-link DNA Tx - Testicular, bladder, ovary, & lung carcinomas AE - Nephrotoxicity, ototoxicity, peripheral neuropathy - prevent nepthrotoxicity w/ amifostine (free radical scavenger) & chloride diuresis
61
Vinblastine | Vincristine
Bind β-tubulin = Inhibit polymerization of microtubules = prevent mitotic spindle formation = cell arrest in metaphase (M-phase) & cell death Tx - Solid tumors, leukemias, & lymphomas AE - VC - neurotoxicity (areflexia, peripheral neuritis) - VB - significant myelosuppression (blasts BM)
62
Paclitaxel Docetaxel (other -taxels)
Hyperstabilize polymerized microtubules in M phase so that mitotic spindle cannot break down (anaphase can't occur) Tx - Ovarian & breast cancers AE - myelosuppression, alopecia, hypersensitivity
63
Etoposide | Teniposide
Inhibits Topoisomerase II = ↑ DNA degredation Tx - Solid tumors (particularly testicular and small cell lung cancer), leukemias, lymphomas AE - myelosuppression, GI irritation, alopecia
64
Irinotecan | Topotecan
Inhibit topoisomerase I = prevent DNA unwinding & replication (S-phase specific) Tx - Colon cancer (I), - Ovarian & small cell lung cancer (T) AE - Severe myelosuppression, diarrhea
65
Hydroxyurea
Inhibits ribonucleotide reductase = ↓ DNA synthesis (S-phase specific) Tx - melanoma, CML - sicle cell disease (↑ HbF) AE - Bone marrow suppression, GI upset
66
Doxorubicin (Adriamycin) Daunorubicin Epirubicin
Intercalate in DNA = breaks in DNA = ↓ replication Generate free radicals Tx - Solid tumors, leukemias, lymphomas AE - Irreversible dilated cardiomyopathy***, myelosuppression, alopecia, toxic to tissues following extravasation Dexrazoxane (iron chelator) helps prevent cardiotoxicity
67
Bleomycin
Induces free radical formation, which causes breaks in DNA strands (causes cell to arrest in G2 phase) Tx - testicular cancer, Hodgkin lymphoma AE - Pulmonary fibrosis (dose-limiting pulmonary toxicity), skin changes, mucositis, limited myelosuppression
68
Dactinomycin (actinomycin D)
Intercalates in DNA Tx - Wilms tumor, Ewing sarcoma, rhabdomyosarcoma - used for childhood tumors (children ACT out) AE - myelosuppression
69
Prednisone | Prednisolone
May trigger apoptosis - even work on nondividing cells Tx - CLL, non-Hodgkin lymphoma (in combo) - immunosuppressants (for autoimmune disease etc.) Most commonly used glucocorticoids in cancer chemotherapy AE - Cushing-like symptoms (weight gain, central obesity, muscle breakdown, cataracts, acne, osteoporosis, hypertension, peptic ulcers, hyperglycemia, psychosis)
70
Tamoxifen | Raloxifene
SERM - receptor antagonists in breast & agonists in bone. Block the binding of estrogen in ER + cells Tx - (T) - breast cancer treatment & prevention - (R) - Prevention of Breast cancer & osteoporosis AE - hot flashes - (T) ↑ risk of endometrial cancer (partial agonist in endometrium) - (R) endometrial antagonist = no ↑ risk of cancer
71
Trastuzumab (Herceptin)
Monoclonal Ab against HER-2 (tyrosine kinase receptor) = helps kill breast cancer cells that overexpress HER-2 through inhibition of HER2-initiated cell signaling & Ab-dependent cytotoxicity Tx - HER-2 + breast cancer & gastric cancer AE - Cardiotoxicity (HEARTceptin) Tras2zumab (HER-2 inhibitor)
72
Imatinib (Gleevac)
Tyrosine kinase inhibitor of bcr-abl (Philadelphia chromosome fusion gene in CML) & c-Kit (common in GI stromal tumors) Tx - CML, GI stromal tumors AE - Fluid retention
73
Rituximab
Monoclonal Ab against CD20, which is found on most B-cell neoplasms Tx - Non-Hodgkin lymphoma, RA (w/ MTX), ITP AE - ↑ risk of progressive multifocal leukoencephalopathy
74
Vemurafenib
Small molecule inhibitor of forms of the B-Raf kinase w/ V600E mutation Tx - metastic melanoma
75
Bevacizumab
Monoclonal Ab against VEGF = Inhibits angiogenesis Tx - Solid tumors (colorectal cancer, renal cell carcinoma) AE - Hemorrhage & Impaired wound healing
76
(Thalidomide)
Inhibit release of VEGF Inhibit IL-6 & TNF-α expression, release & signaling Enhances activity of NK & T cells An important Tx for multiple myeloma AE - Peripheral sensory neuropathy (10-30%) - constipation (commonly)
77
(Interleukin-2)
↑ killing activity of NK cells & ↑ T-cell proliferation Tx - metastatic renal cancers & metastatic melenomas AE - causes intravascular fluid leaks = significant alterations in electrolyte concentrations, cardiac arrhythmias, edema, HoTN, respiratory difficulties, renal failure
78
(Bortezomib)
Small molecule inhibitor of proteosome = prevents proteosomal degradation of p53 Inhibition of transcriptional activity of NF-kB (normally ↑ tumor cell survival in hypoxic environments) Tx - Multiple myeloma (& combo tx in other myelomas) AE - peripheral neuropathy; thrombocytopenia, neutropenia, fatigue, anemia, vomiting, limb pain, dehydration, nausea
79
(tretinoin)
Induces differentiation in APL (acute promyelocytic leukemia) Tx - APL = high rate of complete remission as single agent (can be combined w/ anthracyclines)
80
(Gemcitabine)
Inhibits ribonucleotide reductase = ↓ DNA precursors Incorporated into DNA = inhibit synthesis & function Tx - pancreatic, non-small cell lung, ovarian, bladder & other cancers
81
(Mechlorethamine)
Nitrogen mustard - alkylating agent Tx - Hodgkin's Lymphoma (MOPP = mechlorethamine, vincristine, procarbazine, prednisone)
82
(Anastrazole)
Aromatase Inhibitor = cuts off estrogen supply in post-menopausal women Tx - Estrogen-sensitive breast cancer in post-menopausal women
83
(Flutamide) | Bicalutamide
Competitively inhibit testosterone from binding receptor Tx - prostate cancer

Pharmacology (6 decks)

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