Pharm 1-5

Front 1

Time it takes for amount of drug to fall to half of its value, constant in first order kinetics (majority of drugs)

Back 1

Half-life (T1/2)

Front 2

Relates the amount of drug in the body to the plasma concentration

Back 2

Volume of distribution (VD)

Front 3

Plasma concentration of a drug at a given time

Back 3

Cp

Front 4

The ratio of the rate of elimination of a drug to its plasma concentration

Back 4

Clearance (CL)

Front 5

The elimination of drug that occurs before it reaches the systemic circulation

Back 5

First pass effect

Front 6

The fraction of administered dose of a drug that reaches systemic circulation

Back 6

Bioavailability (F)

Front 7

When the rate of drug input equals the rate of drug elimination

Back 7

Steady state

Front 8

This step of metabolism makes drug more hydrophilic and hence augments elimination

Back 8

Phase I

Front 9

Different steps of Phase I

Back 9

Oxidation, reduction, hydrolysis

Front 10

Products of Phase II conjugation

Back 10

Glucuronate, acetic acid, and glutathione sulfate

Front 11

Inducers of Cytochrome P450

Back 11

Barbiturates, phenytoin, carbamazepine, and rifampin

Front 12

Inhibitors of CYP450

Back 12

Cimetidine, ketoconazole, erythromycin, isoniazid and grapefruit

Front 13

Constant percentage of substrate metabolized per unit time

Back 13

First order kinetics

Front 14

Drug elimination with a constant amount metabolized regardless of drug concentration

Back 14

Zero order kinetics

Front 15

Target plasma concentration multiplied by (volume of distribution divided by bioavailability)

Back 15

Loading dose (Cp*(Vd/F))

Front 16

Concentration in the plasma multiplied by (clearance divided by bioavailability)

Back 16

Maintenance dose (Cp*(CL/F))

Front 17

Strength of interaction between drug and its receptor

Back 17

Affinity

Front 18

Selectivity of a drug for its receptor

Back 18

Specificity

Front 19

Amount of drug necessary to elicit a biologic effect

Back 19

Potency

Front 20

Ability of drug to produce a biologic effect

Back 20

Efficacy

Front 21

Ability of a drug to produce 100% of the maximum response regardless of the potency

Back 21

Full agonist

Front 22

Ability to produce less than 100% of the response

Back 22

Partial agonist

Front 23

Ability to bind reversibly to the same site as the drug and without activating the effector system

Back 23

Competitive antagonist

Front 24

Ability to bind to either the same or different site as the drug

Back 24

Noncompetitive antagonist

Front 25

Mechanism of action (MOA) utilizes intracellular receptors

Back 25

Thyroid and steroid hormones

Front 26

MOA utilizes transmembrane receptors

Back 26

Insulin

Front 27

MOA utilizes ligand gated ion channels

Back 27

Benzodiazepines and calcium channel blockers

Front 28

Median effective dose required for an effect in 50% of the population

Back 28

ED50

Front 29

Median toxic dose required for a toxic effect in 50% of the population

Back 29

TD50

Front 30

Dose which is lethal to 50% of the population

Back 30

LD50

Front 31

Window between therapeutic effect and toxic effect

Back 31

Therapeutic index

Front 32

Drug with a high margin of safety

Back 32

High therapeutic index

Front 33

Drug with a narrow margin of safety

Back 33

Low therapeutic index

Front 34

Antidote used for lead poisoning

Back 34

Dimercaprol, EDTA

Front 35

Antidote used for cyanide poisoning

Back 35

Nitrites

Front 36

Antidote used for anticholinergic poisoning

Back 36

Physostigmine

Front 37

Antidote used for organophosphate and anticholinesterase poisoning

Back 37

Atropine, pralidoxime

Front 38

Antidote used for iron salt toxicity

Back 38

Deferoxamine

Front 39

Antidote used for acetaminophen (APAP) toxicity

Back 39

N-acetylcysteine

Front 40

Antidote for arsenic, mercury, lead, and gold poisoning

Back 40

Dimercaprol

Front 41

Antidote used in poisonings: copper (Wilson's disease), lead, mercury, and arsenic

Back 41

Penicillamine

Front 42

Antidote used for heparin overdose

Back 42

Protamine

Front 43

Antidote used for warfarin toxicity

Back 43

Vitamin K and Fresh frozen plasma

Front 44

Antidote for tissue plasminogen activator (t-PA), streptokinase

Back 44

Aminocaproic acid

Front 45

Antidote used for methanol and ethylene glycol

Back 45

Ethanol

Front 46

Antidote used for opioid toxicity

Back 46

Naloxone (IV), naltrexone (PO)

Front 47

Antidote used for benzodiazepine toxicity

Back 47

Flumazenil

Front 48

Antidote used for tricyclic antidepressants (TCA)

Back 48

Sodium bicarbonate

Front 49

Antidote used for carbon monoxide poisoning

Back 49

100% O2 and hyperbaric O2

Front 50

Antidote used for digitalis toxicity

Back 50

Digi-Bind (also need to stop digoxin, normalize K+, and lidocaine if pt. is arrhythmic)

Front 51

Antidote used for beta agonist toxicity (eg. Metaproterenol)

Back 51

Esmolol

Front 52

Antidote for methotrexate toxicity

Back 52

Leucovorin

Front 53

Antidote for beta-blockers and hypoglycemia

Back 53

Glucagon

Front 54

Antidote useful for some drug induced Torsade de pointes

Back 54

Magnesium sulfate

Front 55

Antidote for hyperkalemia

Back 55

sodium polystyrene sulfonate (Kayexalate)

Front 56

Antidote for salicylate intoxication

Back 56

Alkalinize urine, dialysis

Front 57

Constant proportion of cell population killed rather than a constant number

Back 57

Log-kill hypothesis

Front 58

Treatment with cancer chemotherapy at high doses every 3-4 weeks, too toxic to be used continuously

Back 58

Pulse therapy

Front 59

Toxic effect of anticancer drug can be lessened by rescue agents

Back 59

Rescue therapy

Front 60

Drug used concurrently with toxic anticancer agents to reduce renal precipitation of urates

Back 60

Allopurinol

Front 61

Pyrimidine analog that causes "Thymine-less death" given with leucovorin rescue

Back 61

5-flouracil (5-FU)

Front 62

Drug used in cancer therapy causes Cushing-like symptoms

Back 62

Prednisone

Front 63

Side effect of Mitomycin

Back 63

SEVERE myelosuppression

Front 64

MOA of cisplatin

Back 64

Alkylating agent

Front 65

Common toxicities of cisplatin

Back 65

Nephro and ototoxicity

Front 66

Analog of hypoxanthine, needs HGPRTase for activation

Back 66

6-mercaptopurine (6-MP)

Front 67

Interaction with this drug requires dose reduction of 6-MP

Back 67

Allopurinol

Front 68

May protect against doxorubicin toxic by scavenging free radicals

Back 68

Dexrazoxane

Front 69

Blows DNA (breaks DNA strands), limiting SE is pulmonary fibrosis

Back 69

Bleomycin

Front 70

Bleomycin+vinblastine+etoposide+cisplatin produce almost a 100% response when all agents are used for this neoplasm

Back 70

Testicular cancer

Front 71

MOPP regimen used in Hodgkin's disease (HD)

Back 71

Mechlorethamine+ oncovorin (vincristine)+ procarbazine, and prednisone

Front 72

ABVD regimen used for HD, but appears less likely to cause sterility and secondary malignancies than MOPP

Back 72

Adriamycin (doxorubicin) +bleomycin, vinblastine +dacarbazine

Front 73

Regimen used for non-Hodgkin's lymphoma

Back 73

COP (cyclophosphamide, oncovin(vincristine), and prednisone)

Front 74

Regimen used for breast cancer

Back 74

CMF (cyclophosphamide, methotrexate, and fluorouracil) and tamoxifen if ER+

Front 75

Alkylating agent, vesicant that causes tissue damage with extravasation

Back 75

Mechlorethamine

Front 76

Anticancer drug also used in RA, produces acrolein in urine that leads to hemorrhagic cystitis

Back 76

Cyclophosphamide

Front 77

Prevention of cyclophosphamide induced hemorrhagic cystitis

Back 77

Hydration and mercaptoethanesulfonate (MESNA)

Front 78

Microtubule inhibitor that causes peripheral neuropathy, foot drop (eg. ataxia), and "pins and needles" sensation

Back 78

Vincristine

Front 79

Interact with microtubules (but unlike vinca which prevent disassembly of tubules), it stabilizes tubulin and cells remain frozen in metaphase

Back 79

Paclitaxel (taxol)

Front 80

Toxicities include nephrotoxicity and ototoxicity, leading to a severe interaction with aminoglycosides

Back 80

Cisplatin

Front 81

Agent similar to cisplatin, less nephrotoxic, but greater myelosuppression

Back 81

Carboplatin

Front 82

Converts asparagine to aspartate and ammonia, denies cancer cells of essential AA (asparagine)

Back 82

L-asparaginase

Front 83

Used for hairy cell leukemia; it stimulates NK cells

Back 83

Interferon alpha

Front 84

Anti-androgen used for prostate cancer

Back 84

Flutamide (Eulexin)

Front 85

Anti-estrogen used for estrogen receptor + breast cancer

Back 85

Tamoxifen

Front 86

Aromatase inhibitor used in breast cancer

Back 86

Letrozole, anastrozole

Front 87

Newer estrogen receptor antagonist used in advanced breast cancer

Back 87

Toremifene (Fareston)

Front 88

Some cell cycle specific anti-cancer drugs

Back 88

Bleomycin, vinca alkaloids, antimetabolites (eg., 5-FU, 6-MP, methotrexate, etoposide)

Front 89

Some cell cycle non-specific drugs

Back 89

Alkylating agents (eg., mechlorethamine, cyclophosphamide), antibiotics (doxorubicin, daunorubicin), cisplatin, nitrosourea

Front 90

Anti-emetics used in association with anti-cancer drugs that are 5-HT3 (serotonin receptor subtype ) antagonist

Back 90

Odansetron, granisetron

Front 91

Nitrosoureas with high lipophilicity, used for brain tumors

Back 91

Carmustine (BCNU) and lomustine (CCNU)

Front 92

Produces disulfiram-like reaction with ethanol

Back 92

Procarbazine

Front 93

Somatostatin (SRIF) analog used for acromegaly, carcinoid, glucagonoma and other GH producing pituitary tumors

Back 93

Octreotide

Front 94

Somatotropin (GH) analog used in GH deficiency (dwarfism)

Back 94

Somatrem

Front 95

GHRH analog used as diagnostic agent

Back 95

Sermorelin

Front 96

GnRH agonist used for infertility or different types of CA depending on pulsatile or steady usage respectively

Back 96

Leuprolide

Front 97

GnRH antagonist with more immediate effects, used for infertility

Back 97

Ganirelix

Front 98

Dopamine (DA) agonist (for Parkinson's disease), used also for hyperprolactinemia

Back 98

Bromocriptine

Front 99

Hormone inhibiting prolactin release

Back 99

Dopamine

Front 100

ACTH analog used for diagnosis of patients with corticosteroid abnormality

Back 100

Cosyntropin

Front 101

Synthetic analog of ADH hormone used for diabetes insipidus and nocturnal enuresis

Back 101

Desmopressin (DDAVP)

Front 102

SE of OCs

Back 102

Increased thromboembolic events

Front 103

Most widely used thyroid drugs such as Synthroid and Levoxyl contain

Back 103

L-thyroxine (T4)

Front 104

T3 compound less widely used

Back 104

Cytomel

Front 105

Anti-thyroid drugs

Back 105

Thioamides, iodides, radioactive iodine, and ipodate

Front 106

Thioamide agents used in hyperthyroidism

Back 106

Methimazole and propylthiouracil (PTU)

Front 107

Thioamide less likely to cross placenta, inhibits peripheral conversion of T4 to T3 in high doses, and should be used with extreme caution in pregnancy

Back 107

PTU

Front 108

PTU (propylthiouracil) MOA

Back 108

Inhibits thyroid hormone synthesis by blocking iodination of the tyrosine residues of thyroglobulin

Front 109

Can be effective for short term therapy of thyroid storm, but after several weeks of therapy causes an exacerbation of hyperthyroidism

Back 109

Iodide salts

Front 110

Dose may need to be increased during pregnancy or with Ocs due to increased TBG in plasma

Back 110

Thyroxine

Front 111

Permanently cures thyrotoxicosis, patients will need thyroid replacement therapy thereafter. Contraindicated in pregnancy

Back 111

Radioactive iodine

Front 112

Radio contrast media that inhibits the conversion of T4 to T3

Back 112

Ipodate

Front 113

Block cardiac adverse effects of thyrotoxicosis such as tachycardia, inhibits the conversion of T4 to T3

Back 113

Beta-blockers such as propranolol

Front 114

Vitamins containing iron should NOT be taken simultaneously with levothyroxine because

Back 114

Iron deiodinates thyroxine

Front 115

Thyroxine dose may need to be increased in hypothyroid patient during pregnancy because

Back 115

Estogens increase maternal TBG