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Z5. Pharmacology p329


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p. 329
questions from diagram at bottom of page
plasmin is the major ___________ enzyme. It breaks down both _______ and _______
fibrinolytic enzyme. It accelerates breaks down of both fribin and fibrinogen yielding fibrin splip products and degradation products, respectively.
Fibrinogen is converted to fibrin by _________
tPA and urokinase promote the converson of ______ to ________ thereby increasing fibrinolysis.
plasminogen to plasmin
Various stimuli activate a blood proactivator to a blood activator that promotes conversion of _________ to blank thereby increasing fibrinolysis
plasminogen to plasmin
Streptokinase and anistreplase both activate and Activator that increases convesion of plasminogen to plasmin.
Aminocaproic acid:____________ fibrinolysis.
inhibits fibrinolysis by inhibition of plasminogen conversion to plasmin.
4 examples of thrombolytics include: ________, _________, _____________, and ___________
Streptokinase, urokinase, tPA(altepalse), APSAC (anistreplase)
work by directly or indirectly aiding the conversion of ___________ to __________, which cleaves ______ and ________ clots. tPA specifically coverts _______________ to plasmin
Directly or indirectly aid conversion of plaminogen to plasmin, which cleaves thrombin and fribrin clots. It is claimed that tPA specifically coverts fribrin-bound plasminogen to plasmin.
T/F: clinical use is for DVTs
False: used for early MI
pts. receiving this medication are at most risk for: ______
Hematologic Drugs
p. 330
mechanism of antiplatelet interaction
questions from diagram at top of page
When a break in the endothelium occurs _________ and _________ are exposed.
collagen and vWF
Platelets are activated by binding to the above macromolecules. The two structures expressed by the platelets involved in this process are __________ and _________ and they bind to _________ and __________, repectively
Platelets bind to collagen and vWF. The two structures expressed by platelets that are involved in this process are GP 1a and GP 1b. GP 1a and GP 1b bind to collagen and vWF, respectively.
After platelet activation _________ is expressed on their surface. What is the role of this structure?
after platelets are activated they express GP IIb/IIIa. This molecule is important in platlelet-platelet aggregation.
_________ and _________ interaction is needed in order for platelet aggregation to occur.
GP IIb/IIIa and fribinogen
5-HT, _______, and ________ are molecules that play a role in the glycoprotein expression of activated platelets.
5-HT, ADP, and TxA2 are molecules that play a role in the glycoprotein expression of activated platelets.
Aspirin acts by inhibiting production of ________ that in turn inhibits glycoprotein expression in activated platelets.
ADP production is inhibited by the drug _________.
This antibody drug targets the _______ on platelets.
Copidogrel, ticlopidine
p. 330
T/F: inhibits platele aggregation by irreversibly inhibiting the ADP pathway involved in the binding of fibrinogen
It is used for ______ ________ syndrome, coronary _______, and it has been shown to decrease the incidence or recurrence of___ ____.
it is used for acute coronary syndrome, coronary stenting. Decreases incidence or recurrence of thrombotic stroke
Ticlopidine is associated with_________ as a side effect.
Ticlopidine causes neutropenia and it is reserved for those who cannot tolerate aspirin.
p. 330
This Abciximab binds to __________ on activated platelets.
gp IIb/Iia
Abciximab is used for ___________ and ________ _________ ___________ ___________
acute coronary syndromes and percutanous transluminal coronary angioplasty
Abciximab toxiciites are _______ and ________
bleeding and thrombocytopenia
p 330
It ________ and (reversibly/irreversibly) inhibits COX1 and COX2 to prevent the conversion of _______ to prostaglandins.
acetilates and irreversably inhibits COX-1 and COX-2
T/F: aspirin has an effect of PT, PTT
false it has no effect
What are the 4 A's of aspirin and NSAIDS in general
Antipyretic, Analgesic, Anti-inflam, antiplatelet
Important toxicities include _________, bleeding, hyperventilation, __________- in children, and CN ____ toxicity
gastric ulceration, bleeding, hyperventilation, Reyes syndrome and tinnitus (CNVIII).
Endocrine Drugs
pg 332
diabetes drugs
Marc Waase
Hydrocortisone, prednisone, triamcinolone, dexamtasone, bleclomethasone are examples of what kind of drugs?
Glucocorticoids decrease the production of ___ and ____
Leukotrienes and prostanglandins
To treat Addison's disease, inflammation, immune suppression, asthma, use ____
An important side-effect of Glucocortioid usage is ____
Iatrogenic Cushing's Syndrome
Buffalo hump, moon facies, truncal obesity, muscles wasting, thin skin, easy bruisability, osteoporosis, adrenocortical atrophy, peptic ulcers characterize what syndrome?
Cushing's Syndrome
Reproductive Drugs
pg 332
Which two drugs inhibit cGMP phosphodiesterase, leading to smooth muscle relaxation in the corpus cavernosum and penile erection?
Sildenafil and Verdenafil --they fill the penis
What class of drugs are used tto treat erectile dysfunction
cGMP Inhibitors
CGMP inibitors taken with ____have a high risk of liofe-threeatening hypotension
Which drugs is a partial agonist of estrogen recpetors in the pituitary gland, stimulating increase in LH and FSH, which stimulates ovulation to treat infertility
Clomiphene's side effects include:
Hotflashes, ovarian enlargment, multiple simultaneous pregnancies, visual disturbances
What abortifacient is a competitite inhibitor of preogestins at progesterone recpetor and may lead to heavy menstrual-like bleeding?
Mifepristone (RU486)
The advantage of this drug is that it is reliable, decreases incidence of ectopic pregnancy, decreases risk of pelvic infections, and regulates menses; however it also puts you in a hypercoagulable stat and may increase your trigylcerides, weight, and bl
Oral Contracpetices - syntheitc progestins/estrogen
Rheumatologic Drugs
pg 333
____is converted to uric acid which leads to gout
Xanthine (converted from excess purines)
This drug depolymerizes microtubules, impairing leukocyte chemotaxis and degranulation, and used to treat acute gout
This drugs inhibits reabsorption of uric acid and used to treat chronic gout
This drug is used to treat chronic gout, but also inhbits secretion of penicillin
This drugs inhibits xanthine oxidase decreasing the conversion fo xanthine to uric acid
Oncologic Drugs
pg 333-336
What are the cell cycle specific oncologic drugs
antimetabolites, plant alkaloids, stroid hormones, bleomycin, paclitaxel, etoposide
What are the cell cycle Nonspecific oncologic drugs?
alkylating agents and antibiotics
____is an S-phase-specific anti-metabolite that is an folic acid analog that inhibits dihydrofolate reducate decreasing dTMP(thymidine and purines) and decreaing DNA/prtein synthesis.
____is an S-phase-specific anti-metabolite that is a pyrmidine analog which complexed to folic acid, inhibiting thymidylate synthase, decreasing dTMP and decreasing DNA/protein synthesis
5-Fluorouracil (5-FU)
Myelosuppression by methotrxate is reversible with ____
leucovorin (folinic acid) rescue
Which drug blocks purine synthesis and is used to treat leukemias, lymphomas (not CLL or Hodgkins)
6-mercaptopurine (6-MP)
Which drug alkylates DNA and is used to treat CML?
Which drug inhibits DNA polymerase and is used to treat AML?
This drug used to treat Leukemias and Lymphomas is metaboilized by xanthine oxidase
6-mercaptopurine (6-MP)
Used to treat leukemias, lymphomas, choricarcinoma, sacromas, rheumatoid arthritis, psoriasis, and can be an abortifacient; it may lead to myelosuppression
Used to treat colon cancer and other solid tumors, basal cell carcinoma (topically)
5-Fluorouracil (5-FU)
Myelosuppression by 5-FU is ______
Not reversible
This drug used to treat AML may lead to leukopenia, thrombocytopenia, megaloblastic anemia?
This drugs used to treat CML may lead to pulmonary fibrosis and hyperpigmentation?
____is an alkylating agent acivated by liver that covalently x-links DNA at guanine N-7, and is used to treat non-hodgkin's lymphoma, breast/ovarian carcinomas
____ alkylates DNA after bioactivation and can cross the BBB and treats brain tumors (glioblastoma multiforme)
Nitrosoureas (Carmustine, lomustine, semustine, streptozocin)
____acts like an alkylating agent, x-linking via hyrdolysis of Cl and platinum; used to treat testicular, bladder, lung carcinomas
This alkylating agent can cause myelosuppression and hemorhagic cystitis
This combination of drugs is used to treat Hodgkin's and myelomas, sarcomas, and solid tumors (breast, ovary, lung)
ABVD: Adriamycin, Bleomycin, Vinblastine, Dacarbazine
____noncovalently intercalates in DNA, creating breaks to decrease replication and transcription
Doxorubicin (adriamycin)
____intercalates DNA strands and induces free radical fromation which causes strand breaks
Bleomycin, Dactinomycin
Which drugs causes cardiotoxicity, alopecia, and myelosuppression?
Doxorubicin (adriamycin)
Which drug is used to trat oat cell carcinoma of the lung and prostate/testicular carcinoma?
This combination of drugs is used to treat lymphoma, CLL, Hodgkin's, Wilm's tumor, choriocarcinoma
MOPP (Mustargen, Oncovin (Vincristine), Procarbazine (Matulane), Prednisone)
Which glucocorticoid may trigger apoptosis and may even work on nondividing cells
This drug is a G2-phase specific inhibitor of Topisiomerase II, leaving double strand breaks in DNA following DNA replication
This drug used to treat testicular cancer and lymphomas may cayse pulmonary fibrosis, skin chnages, and myelosuppression
Bleomycin, Dactinomycin
This drugs used as an immunosuppressant and in lymphomas may cause acne, osteoporosis, hypertension, peptic ulcers, hyperglycemia, psychosis?
____is an estrogen receptor mixed agonist/antagonist that blocks the binding of estrogen to ER+ cells.
____is n M-phase-specific alkaloid that binds to tubulin and blocks polymerization of microtubules, preventing spindle formation
Vincristine and Vinblastine
____is an M-phase-specific agen that binds to tubulin and hyperstabilizes the polymerized microtubules, so that the mitotic spindle cannot break down
What drugs is used to treat breast cancer, but may increas the risk of endometrial carcinomas and hot flashes
Side-effects of Vinblastine includeÂ….
VinBASTine BLASTs Bone Morraow, causing myelosuppression, as well as neurotoxicity and paralutic ileus.
Side effects of Paclitaxel includeÂ….
Myelosuppression and hypersensitivity
Immunosuppressants and Cytokine Therapy
pg 336-337
This drug binds to cyclophilins, blocking differentiation and activation of T cells mainly by inhibiting IL2 production
This antimetabolite derivative of 6-mercaptopurine interferes with the metabolism and synthesis of nucleic acid, therefore toxic to proliferating lymphocytes
This potent immunosuppressive drug binds to the FK-binding protein and inhibits secretion of IL2 and other cytokines
tacrolimus (FK506)
This drug is used to suppress organ rejection after transplantation, but may predispose patient to viral infections and lymphoma
Azaothioprine is used to in what setting?
Kidney transplants, autoimmune disorders (glomerulonephritis, hemolytic anemia)
Recombinant Cytokine- Aldesleukin (interleukin-2) is used for?
Renal cell carcinoma, metastatic melanoma
Recombinant Cytokine- Erythropoietin (epoetin) is used for?
Recombinant Cytokine- Filgrastim is used for?
Recovery of Bone Marrow; it is a granulocyte colony stimulating factor
Recombinant Cytokine- alpha interferon is used for?
Hep B/C, Kaposi's sarcoma, leukemia, malgnant melanoma
Recombinant Cytokine- beta interferon is used for?
Multiple Sclerosis
Recombinant Cytokine- gamma interferon is used for?
Chronic Granulomatous disease
Recombinant Cytokine- oprelvekin (interleukin2) is used for?
Recombinant Cytokine- sargamostim is used for?
Recovery of Bone Marrow (it is a granulocyte-macrophage colony stimulating factor)
Recombinant Cytokine- thrombopoietin is used for?
pg 338
What is the antidote for acetaminophen toxicity/overdose
What is the antidote for salicylates toxicity/overdose
Alkanize urine/dialysis
What is the antidote for antichoinesterase toxicity/overdose
Atropine, pralidoxime
What is the antidote for antimuscarinic/anticholinergic agents toxicity/overdose
physostigimine salicylate
What is the antidote for Beta-blockers toxicity/overdose
What is the antidote fordigitalis toxicity/overdose
Stop digitalis, Normalize K+, lodpcaine, anti-digitialis Fab Fragments, Magnesium
What is the antidote for lead toxicity/overdose
CaEDTA, dimercaprol, succimer, penicillamine
What is the antidote for iron toxicity/overdose
What is the antidote for aresnic/mercury/gold toxicity/overdose
Dimercaprol (BAL), succimer
What is the antidote for copper, arsenic, gold toxicity/overdose
What is the antidote N-acetylcysteine used to treat?
Acetaminophen toxicity/overdose
What is the antidote for cyanide toxicity/overdose
nitrite, hydroxocobalamin, thiosoulfate
What is the antidote for methemoglobin toxicity/overdose
methylene blue
What is the antidote glucagon used to treat?
Beta-blocker toxicity/overdose
What is the antidote for carbon monoxide toxicity/overdose
100% oxygen, hyperbaric oxygen
What is the antidote atropine used to treat?
anticholinesterase toxicity/overdose
What is the antidote for methanol toxicity/overdose
Ethanol, dialusis, fomepizole
What is the antidote for opiods toxicity/overdose
What is the antidote for ethylene glycol toxicity/overdose
Ethanol, dialusis, fomepizole
What is the antidote for benzodiazepines toxicity/overdose
What is the antidote for (TCA) Tricyclic Antidepressants toxicity/overdose
What is the antidote for Heparin toxicity/overdose
What is the antidote Deferoxamine used to treat?
Iron toxicity/overdose
What is the antidote for warfarin toxicity/overdose
vitamin K, fresh frozen plasma
What is the antidote Naloxone/naltrexone used to treat?
opioid toxicity/overdose
What is the antidote for tPA/streptokinase toxicity/overdose
aminocaproic acid
What is the antidote Physostigmine salicylate used to treat?
Antimuscarinic/anticholinergic agents toxicity/overdose
What is the antidote Flumazenil used to treat?
Benzodiazepine toxicity/overdose
What is the antidote Protamine used to treat
Heparin toxicity/overdose
Children living in old houses might eat the paint chips which could cause ____
Lead Poisoning
Signs of Lead poisoning include:
Lead Lines on gingivae and epiphyses of Long bones, Encephalopathy and Erythrocyte Basophilic stippling, Abdominal colic and sideroblastic Anemia, Wrist and Foot Drop
1st line of Treatment for Lead Poisoning include
Dimercaprol and EDTA
Weak acids, such as phenobarbitol, methotreaxate, aspirin, alkanize urine with ____ to increase clearance
Weak bases, such as amphetamines, acidify urine with NH4Cl to ____ clearance
Drug reactions
p. 339
For each drug reaction, give the pharmacological agents responsible. The number of drugs you should list are given in parentheses. You could also quiz yourself in reverse by going down the list of drugs on the right.
Pulmonary fibrosis (3)
bleomycin, amiodarone, busulfan
Hepatitis (2)
isoniazid, halothane
Focal to massive hepatic necrosis (4)
halothane, valproic acid, acetaminophen, amanita phalloides
Anaphylaxis (1)
SLE-like syndrome (4). [mnemonic: it's not HIPP to have lupus]
hydralazine, INH, procainamide, phenytoin
Hemolysis in G6PD-deficient patients (8)
sulfonamides, INH, aspirin, ibuprofen, primaquine, nitrofurantoin, pyrimethamine, chloramphenicol
Thrombotic complications (1 class)
OCPs (e.g. estrogens and progestins)
Adrenocortical insufficiency (withdrawal of what class of drugs causes adrenocortical insufficiency?)
withdrawal of glucocorticoids causes hypothalamic-pituitary-axis suppression
Photosensitivity reactions (3) [mnemonic: SAT for a photo]
Sulfonamides, amiodarone, tetracycline
Induce P-450 system (6)
barbiturates, phenytoin, carbamazepine, rifampin, griseofulvin, quinidine
Inhibit P-450 system (6, including one fruit)
cimetidine, ketoconazole, grapefruit, erythromycin, INH, sulfonamides
Tubulointerstitial nephritis (5)
sulfonamides, furosemide, methicillin, rifampin, NSAIDs (except aspirin)
Hot flashes (1)
Cutaneous flushing (4)
niacin, Ca++ channel blockers, adenosine, vancomycin
Cardiac toxicity (2)
doxorubicin (adriamycin), daunorubicin
Agranulocytosis (3, all start with letter C)
clozapine, carbamazepine, colchicine
Stevens-Johnson syndrome (3)
ethosuximide, sulfonamides, lamotrigine
Cinchonism (2)
quinidine, quinine
Tendonitis, tendon rupture and cartilage damage (kids) (1)
Disulfiram-like reaction (4)
metronidazole, certain cephalosporins, procarbazine, sulfonylureas
Otoxicity and nephrotoxicity (3)
aminoglycosides, loop diuretics, cisplatin
Drug-induced Parkinson's (4)
haloperidol, chlorpromazine, resperine, MPTP
Torsades de pointes (two subclasses of antiarrhythmics)
Class III (sotalol), class IA (quinidine) antiarrhythmics
Aplastic anemia (3)
chloramphenicol, benzene, NSAIDs
Neuro/nephrotoxicity (1)
Pseudomembranous colitis (2)
clindamycin, ampicillin
Gynecomastia (5) [mnemonic: Some Drugs Create Awesome Knockers]
spironolactone, digitalis, cimetidine, chronic Alcohol use, estrogens, ketoconazole
Atropine-like side effects (1)
Cough (1)
ACE inhibitors (losartan --> no cough)
Gingival hyperplasia (1)
Diabetes insipidus (1)
Tardive dyskinesia (1)
Fanconi's syndrome (1)
Gray baby syndrome (1)
Extrapyramidal side effects (3)
chlorpromazine, thioridazine, haloperidol
Osteoporosis (2)
corticosteroids, heparin
Alcohol toxicity
p. 340
Ethylene glycol is converted to ------- ------ by alcohol dehydrogenase. This product can lead to acidosis and nephrotoxicity.
oxalic acid.
Alcohol dehyrogenase also converts methanol to formaldehyde and formic acid, which can cause severe ----- and damage to the -------.
acidosis. retina
Ethanol competes with ethylene glycol and methanol (if present) for alcohol dehydrogenase. ADH action on EtOH produces -------.
What symptoms does acetaldehyde cause?
nausea, vomiting, headache, hypotension
Acetaldehyde itself can be metabolized by acetaldehyde dehydrogenase to ----- -----.
acetic acid.
Acetaldehyde dehydrogenase is inhibited by what drug?
Herbal agents
p. 341
Give the clinical uses for the following herbal agents.
GI distress, dizziness, and headache
CNS and cardiovascular stimulation; arrhythmias, stroke and seizures at high doses.
GI distress, mouth ulcers, antiplatelet actions
GI distress, anxiety, insomnia, headache, and antiplatelet actions
GI distress, sedation, ataxia, hepatotoxicity, phototoxicity, dermatotoxicity
milk thistle
loose stools
saw palmetto
GI distress, decreased libido, hypertension
St. John's wort
GI distress and phototoxicity; serotonin syndrome with SSRIs
Androgenization (premenopausal women), estrogenic effects (postmenopausal), feminization (young men)
Sedation, suppresses midcycle LH, hypoprolactinemia
Give the toxicities for the following herbal agents.
Drug name
p. 341
For each drug name ending, give the general category of drug it indicates and an example of a drug in that category.
inhalational general anesthetic. Halothane
benzodiazepine. Diazepam
phenothiazine (neuroleptic, antiemetic). Chlorpromazine
antifungal. Ketoconazole
barbiturate. Phenobarbital
local anesthetic. Lidocaine
penicillin. Methicillin
antibiotic, protein synthesis inhibitor. Tetracycline
tricyclic antidepressant. Imipramine
protease inhibitor. Saquinavir
beta antagonist. Propranolol
butyrophenone (neuroleptic). Haloperidol
cardiac glycoside (inotropic agent). Digoxin
methylxanthine. Theophylline
ACE inhibitor. Captopril
beta-2 agonist. Albuterol
H2 antagonist. Cimetidine
tricyclic antidepressant. Amitriptyline
pituitary hormone. Somatotropin
alpha-1 antagonist. Prazosin

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