Unstarred - Deck 1 Flashcards by Rex David

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

Volume of distribution (VD)

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Plasma concentration of a drug at a given time

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

Clearance (CL)

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

First pass effect

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The fraction of unchanged drug that reaches systemic circulation after administration

Bioavailability (F)

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

Steady state

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Different steps of Phase I

Hydrolysis
Oxidation
Reduction

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Name 3 Phase II conjugation reactions

Acetylation
Glucuronidation
Glutathione conjugation
Glycine conjugation
Methylation
Sulfation 
Water conjugation

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Constant percentage of drug metabolized per unit time

First order kinetics

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Constant amount of drug metabolized per unit time

Zero order kinetics

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

Loading dose 
(Cp*(Vd/F))

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Concentration in the plasma times (clearance divided by bioavailability)

Maintenance dose 
(Cp*(CL/F))

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Strength of interaction between drug and its receptor

Affinity

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Selectivity of a drug for its receptor

Specificity

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Amount of drug necessary to elicit a biologic effect compared with another drug

Potency

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A drug with ability to produce maximal response after binding to the receptor is called a?

Full agonist

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A drug with the ability to produce less than maximal response after binding to the receptor is called a?

Partial agonist

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A drug with the ability to bind reversibly to the same site as the drug and without activating the effector system is called a?

Competitive antagonist

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A drug that has the ability to bind irreversibly to the active site or bind to a site distinctly separate from the agonist binding site is called a?

Noncompetitive antagonist

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ACh and Nicotine use what mechanism of action (MOA)?

Ligand gated ion channels

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Dose which produces therapeutic response in 50% of the poopulation

ED50

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Dose which is toxic in 50% of the population

TD50

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Dose which is lethal to 50% of the population

LD50

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Window between therapeutic effect and toxic effect

Therapeutic index

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Drugs that have a high margin of safety are indicated by:

High therapeutic index

Drugs that have a narrow margin of safety are indicated by:

Low therapeutic index

Antidotes used for lead poisoning (without encephalopathy)

Dimercaprol Edetate calcium disodium Succimer

Antidotes used for cyanide poisoning

Nitrites, Hydroxocobalamin (cyanokit) Sodium thiosulfate ("NHS would need to look into cyanide poisoning outbreak")

Antidote used for anticholinergic poisoning

Physostigmine

Antidote used for iron salt toxicity

Deferoxamine

Antidote for severe lead poisoning (with encephalopathy)

Dimercaprol AND CaEDTA (edetate calcium disodium)

Antidote for arsenic, mercury, and gold poisoning

Dimercaprol

Antidote used in Wilson's disease (copper poisoning)

Penicillamine

Antidote used for methanol and ethylene glycol toxicity

Ethanol

Antidote used for tricyclic antidepressants (TCA)

Sodium bicarbonate

Antidote used for carbon monoxide poisoning

100% O2 and hyperbaric O2

Antidote used for digitalis toxicity

Digibind | If pt. is arrhythmic, you would also need to d/c digoxin, normalize K+, and give Lidocaine

Antidote used for beta agonist toxicity (eg. Metaproterenol)

Esmolol

Antidote for methotrexate toxicity

Leucovorin

Antidote for beta-blocker overdose and hypoglycemia

Glucagon

Antidote useful for some drug induced Torsade de pointes

Magnesium sulfate

Antidote for hyperkalemia

Sodium Polystyrene Sulfonate [KAYEXELATE]

Methods to reduce salicylate intoxication

Alkalinize urine | Dialysis

When the constant proportion of cell population killed rather than a constant number, it is called?

Log-kill hypothesis

Name the treatment with cancer chemotherapy at high doses every 3-4 weeks, too toxic to be used continuously.

Pulse therapy

Name the treatment when toxic effect of anticancer drug can be lessened by rescue agents.

Rescue therapy

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

Allopurinol

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

5-Fluorouracil (5-FU)

Drug used in cancer therapy causes Cushing-like symptoms

Prednisone

Side effect of Mitomycin

SEVERE myelosuppression

MOA of cisplatin

Alkylating agent

Common toxicities of cisplatin

Nephrotoxicity Ototoxicity "Say NO to Cisplatin"

Analog of hypoxanthine, needs HGPRTase for activation

6-mercaptopurine (6-MP)

MOPP regimen used in Hodgkin's disease (HD)

Mechlorethamine Oncovorin (vincristine) Procarbazine Prednisone

Regimen used for non-Hodgkin's lymphoma

``` CHOP Cyclophosphamide Oncovin (vincristine) Doxorubicin Prednisone) ``` + Rituximab (rituxan)

Regimen used for breast cancer

(CMF) Cyclophosphamide Methotrexate Ffluorouracil (and tamoxifen if ER+)

Alkylating agent, vesicant that causes tissue damage with extravasation

Mechlorethamine

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

Cyclophosphamide

Measures to prevent Cyclophosphamide-induced Hemorrhagic Cystitis

Hydration | Mercapto-ethane-sulfonate (MESNA)

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

Vincristine

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

Cisplatin

Agent similar to cisplatin, less nephrotoxic, but greater myelosuppression

Carboplatin

Enzyme that converts asparagine to aspartate and ammonia, denies cancer cells of essential AA (asparagine)

L-asparaginase

Used for hairy cell leukemia; it stimulates NK cells

Interferon alpha

Anti-androgen used for prostate cancer

Flutamide (Eulexin)

Cell Cycle Specific anti-cancer drugs

Antimetabolites (eg., 5-FU, 6-MP, methotrexate, etoposide) Bleomycin Vinca alkaloids

Cell Cycle Non-Specific drugs

Alkylating agents (eg., mechlorethamine, cyclophosphamide) Anthracyclines (Doxorubicin, daunorubicin) Cisplatin Nitrosourea

Nitrosoureas with high lipophilicity, used for brain tumors

Carmustine (BCNU) and lomustine (CCNU)

Alkylating agent that produces disulfiram-like reaction with ethanol

Procarbazine

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

Octreotide

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

Somatrem

GHRH analog used as diagnostic agent

Sermorelin

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

Leuprolide

GnRH antagonist with more immediate effects, used for infertility

Ganirelix

An isomer of T3 which may be used in myxedema coma

Liothyronine (T3)

Anti-thyroid drugs

Thioamides (methimazole, propylthiouracil - PTU) Potassium iodide Radioactive iodine (131I)

Thioamide agents used in hyperthyroidism

Methimazole | Propylthiouracil (PTU)

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

Iodide salts (potassium iodide)

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

Radioactive iodine

Used for the symptomatic treatment of thyrotoxicosis by blocking cardiac adverse effects

Beta-blockers (e.g. Propranolol, Esmolol)

3 zones of adrenal cortex and their products

Glomerulosa (mineralocorticoids) Fasciculata (glucocorticoid=GC) Reticularis (adrenal androgens)

Mnemonic for 3 zones of adrenal cortex

GFR

Used for Addison's disease, Congenital Adrenal Hyperplasia (CAH), inflammation, allergies, and asthma (as a local inhalation)

Glucocorticoids

Short acting GC's

Cortisone | Hydrocortisone (Cortisol equivalent)

Intermediate acting GC's

``` Fluprednisone Methylprednisolone Oaramethasone Prednisone, Prednisolone Triamcinolone ```

Long acting GC's

Betamethasone Dexamethasone Paramethasone

Mineralocorticoids

Deoxycorticosterone | Fludrocortisone

Period of time of therapy after which GC therapy will need to be tapered

5-7 days

Used for Cushing's syndrome (increased corticosteroid) and sometimes for adrenal function test

Metyrapone

Inhibits conversion of cholesterol to pregnenolone therefore inhibiting corticosteroid synthesis

Aminoglutethimide

Antifungal agent used for inhibition of all gonadal and adrenal steroids

Ketoconazole

Antiprogestin used as potent antagonist of GC receptor

Mifepristone

Slightly increased risk of breast cancer, endometrial cancer, heart disease (questionable), has beneficial effects on bone loss

Estrogen

Antiestrogen drugs used for fertility and breast cancer respectively

Clomiphene | Tamoxifen

Common SE of tamoxifen and raloxifene

Hot flashes

Estrogens mostly used in oral contraceptives (OC)

Ethinyl estradiol | Mestranol

Anti-progesterone used as abortifacient

Mifepristone (RU-486)

Constant low dose of estrogen and increasing dose of progestin for 21 days (last 5 days are sugar pills or iron prep)

Combination oral contraceptives (OC)

Oral contraceptive available in a transdermal patch

Ortho-Evra

5 alpha-reductase inhibitor used for benign prostatic hyperplasia (BPH) and male pattern baldness

Finasteride (Proscar) | Propecia

Anabolic steroids that have potential for abuse

Nandrolone | Stanozolol

Anti-androgen used for hirsutism in females

Cyproterone acetate

Alpha cells in the pancreas do what?

Produce glucagon

Beta cells in the pancreas do what?

Produce insulin

Beta cells are found where?

Islets of Langerhans

Delta cells in the pancreas do what?

Produce Somatostatin

A form of endogenous insulin

Normal C-peptide

Very rapid acting insulin, having fastest onset and shortest duration of action

Lispro (Humalog)/Apidra (glulisine)

Rapid acting, crystalline zinc insulin used to reverse acute hyperglycemia

Regular (Humulin R)

Ultra long acting insulin, has over a day duration of action

Glargine (Lantus)

Major side effect of insulin

Hypoglycemia

What receptor is important in synthesis of glucose to glycogen in the liver?

GLUT 2

What receptor is important in muscle and adipose tissue for glucose transport across muscles and TG storage by lipoprotein lipase activation

GLUT 4

Examples of alpha-glucosidase inhibitors (AGI)

Acarbose | Miglitol

MOA of Alpha Glucosidase Inhibitors (AGI's)

Act on intestine, delay absorption of glucose

SE of Alpha Glucosidase Inhibitors (AGI's)

Abdominal cramps Flatulence (DO NOT use Beano to tx) Diarrhea

Alpha-glucosidase inhibitor associated with elevation of LFT's

Acarbose

MOA of nateglinide

Stimulates rapid and transient release of of insulin through closure of the ATP-sensitive K+ channel

Example of a Biguanide

Metformin

Drugs available in combination with metformin

``` Acroplus Met progutazone and metformin Janumet and Janumet XR Sitagliptin and Metformin Glyburide Glipizide Rosiglitazone ```

MOA of metformin

Decreases hepatic glucose production and intestinal glucose absorption; increases insulin sensitivity

Most important potential SE of metformin

Lactic acidosis

Example of a Meglitinide

Repaglinide

MOA of repaglinide

Stimulates insulin release from pancreas; faster and shorter acting than sulfonylurea

First generation sulfonylureas

Chlorpropamide Tolazamide Tolbutamide etc.

Second generation sulfonylureas

Glimepiride Glipizide Glyburide "Put your pride aside and go for a ride"

MOA of both generations of Sulfonylureas

Promotes Insulin release from pancreas by modifying K+ channels

Common SE of sulfonylureas, repaglinide, and nateglinide

Hypoglycemia

Sulfonylurea NOT recommended for elderly because of very long half life

Chlorpropamide

Thiazolidinediones

Pioglitazone Rosiglitazone Troglitazone (withdrawn/d from market)

Reason troglitazone was withdrawn from market

Hepatic toxicity

MOA of thiazolindinediones

Stimulate PPAR-gamma receptor to regulate CHO and lipid metabolism

SE of Thiazolindinediones

``` Anemia (mild) Bladder Cancer (if used >1yr) CHF (worsening if already present Edema Interaction w/ drugs that undergo CytP450 3A4 metabolism ```

Hyperglycemic agent that increases cAMP and results in glycogenolysis, gluconeogenesis, reverses hypoglycemia, also used to reverse severe beta-blocker overdose and smooth muscle relaxation

Glucagon

Available bisphosphonates

``` Alendronate Etidronate Pamidronate Risedronate Tiludronate Zoledronic Acid ```

MOA of Bisphosphonates

Inhibits osteoclast bone resorption

Uses of bisphosphonates

Osteoporosis Paget's disease Osteolytic bone lesions Hypercalcemia from malignancy

Major SE of bisphosphonates

Chemical esophagitis

Bisphosphonates that cannot be used on continuous basis because it caused osteomalacia

Etidronate

Used for prevention of postmenopausal osteoporosis in women

Calcium regulators: Bisphosphonates (Alendronate, Ibandronate, Risedronate) Estrogen (HRT-Hormone replacement therapy)

Drug used especially in postmenopausal women, dosage should be 1500 mg

Calcium

Vitamin given with calcium to ensure proper absorption

Vitamin D

Disease caused by excess ergot alkaloids

St. Anthony's Fire

A class of endogenous substances that include histamine, serotonin, prostaglandins, and vasoactive peptides that work in autocrine or paracrine manner

Autacoids

Syndrome of hypersecretion of gastric acid and pepsin usually caused by gastrinoma; it is associated with severe peptic ulceration and diarrhea

Zollinger-Ellison Syndrome

1st generation antihistamine that is least sedating

Chlorpheniramine

Generation of antihistamine that has the most CNS effects

First generation (d/t being more lipid-soluble)

Major indication for H1 receptor antagonist

Use in IgE mediated allergic reaction (allergic rhinitis, urticaria)

Antihistamine that is indicated for allergies, motion sickness, and insomnia

Diphenhydramine

H1 antagonist used in motion sickness

Dimenhydrinate and other 1st generation

Most common side effect of 1st generation antihistamines

Sedation, anticholinergic

Clinical use for H2 blockers

Acid reflux disease Duodenal ulcer Peptic Ulcer Disease

Receptors for serotonin (5HT-1) are located? What do they do?

Mostly in the brain, and they mediate synaptic inhibition via increased K+ conductance

Triptan available in parenteral and nasal formulation

Sumatriptan

H1 blocker that is also a serotonin antagonist

Cyproheptadine

5HT2 antagonists that mediate synaptic excitation in the CNS and smooth muscle contraction

Cyproheptadine Ergot alkaloids (partial agonist of alpha and serotonin receptors) Ketanserin

5ht-3 antagonist that has been MOST associated with QRS and QTc prolongation and should not be used in patients with heart disease

Dolasetron

Drug used in ergot alkaloids overdose, ischemia and gangrene

Nitroprusside

Reason ergot alkaloids are contraindicated in pregnancy

Cause uterine contractions

SE of ergot alkaloids

Hallucinations resembling psychosis

Peptides causing increased capillary permeability and edema

Bradykinin | Histamine

Difference between COX 1 and COX 2 "

COX 1 is constitutive (expressed in most tissues) | COX 2 may be induced during inflammation (but is constitutive in some tissues)

Drug that selectively inhibits COX 2

Celecoxib

Major SE of zileuton

Liver toxicity

Inhibitor of leukotrienes (LTD4) receptors and used in asthma

Zafirlukast and montelukast

Approved for use in severe pulmonary HTN

PGI2 (epoprostenol)

Irreversible, nonselective COX inhibitor

Aspirin (or other salicylates)

Class of drugs that reversibly inhibit COX

NSAIDS

Primary endogenous substrate for Nitric Oxidase Synthase

Arginine

Long acting beta 2 agonist used in asthma

Salmeterol

Enzyme which theophylline inhibits

Phosphodiesterase

Methylxanthine derivative used as a remedy for intermittent claudication

Pentoxifylline

Antidote for severe CV toxicity of theophylline

Beta blockers

MOA of corticosteroids

Induce lipocortins to 1. inhibit phospholipase A2 2. repress COX-2 gene and enzyme expression 3. repress cytokines that activate COX-2

MOA of penicillin

Block cell wall synthesis by inhibiting transpeptidase and block peptidoglycan cross-linkage

Type of resistance found with vancomycin

Point mutation

Two toxicities of aminoglycosides

Nephrotoxicity | Ototoxicity

Drug of choice for Legionnaires' disease

Azithromycin (or macrolides)

Penicillins active against penicillinase secreting bacteria

Methicillin, nafcillin, and dicloxacillin

Class of antibiotics that have 10% cross sensitivity with penicillins

Cephalosporins

PCN active against pseudomonas

Carbenicillin, piperacillin and ticarcillin

Antibiotic causing Red-Man Syndrome, and prevention measures for syndrome?

Vancomycin, can be prevented by infusion at a slow rate and antihistamines

Drug causes teeth discoloration

Tetracycline

Mechanism of action of tetracycline

Decreases protein synthesis by binding to 30S ribosome and prevent binding of tRNA to A site

Drug that causes gray baby syndrome and aplastic anemia

Chloramphenicol

Drug notorious for causing pseudomembranous colitis

Clindamycin

Treatment of resistant pseudomembranous colitis

Vancomycin PO

Reason fluoroquinolones are contraindicated in children and pregnancy

Cartilage damage

Metronidazole SE if given with alcohol

Disulfiram-like reaction

MOA of nystatin

Bind ergosterol in fungal cell membrane

Neurotoxicity with isoniazid (INH) prevented by

Administration of Vit. B6 (pyridoxine)

Main toxicity of amphotericin

Nephrotoxicity

SE seen only in men with administration of ketoconazole

Gynecomastia

Topical DOC in impetigo

Topical mupirocin (Bactroban)

DOC for CMV retinitis

Ganciclovir

SE for ganciclovir

Myelosuppression

Anti-viral agents associated with Steven Johnson syndrome

Nevirapine | Amprenavir

Antivirals that are teratogens

Delavirdine Efavirenz Ribavirin

Antivirals associated with neutropenia

Ganciclovir Interferon Saquinavir Zidovudine

HIV med used to reduce transmission during birth

AZT (zidovudine)

Drug used for African sleeping sickness

Suramin

Drug used in Chagas disease

Nifurtimox

Cephalosporins able to cross the BBB

Cefixime (2nd) and 3rd generation

Cephalosporins that cause kernicterus in neonates

Ceftriaxone | Cefuroxime

SE of INH

Peripheral neuritis | Hepatitis

Aminoglycoside that is least ototoxic

Streptomycin

Drug used in exoerythrocytic cycle of malaria

Primaquine

Oral antibiotic of choice for moderate inflammatory acne

Minocycline

Drug of choice for leprosy

Dapsone

Mechanism of action of macrolides (erythromycin, clarithromycin)

Inhibit protein synthesis by binding to domain V of 23S rRNA of 50S ribosome subunit

Antibacterials for optimal treatment of acute uncomplicated cystitis

Nitrofurantoin [MACROBID] Trimethoprim-sulfamethoxazole [BACTRIM] Fosfomycin

Antibacterials for optimal treatment of acute pyelonephritis

Fluoroquinolones (Ciprofloxacin, Levofloxacin) | Trimethoprim-sulfamethoxazole [BACTRIM]

Lactam that can be used in PCN allergic patients

Aztreonam

SE of imipenem

Seizures

Anti-viral with a dose limiting toxicity of pancreatitis

Didanosine

Common side effect of hypnotic agents

Sedation

Occurs when sedative hypnotics are used chronically or at high doses

Tolerance

The most common type of drug interaction of sedative hypnotics with other depressant medications

Additive CNS depression

Major effect of benzodiazepines on sleep at high doses

REM is decreased

Neurologic SE of benzodiazepines

Anterograde amnesia

Main route of metabolism for benzodiazepines

Hepatic

Benzodiazepine that undergo extrahepatic conjugation (which are useful in older or hepatically impaired)

Lorazepam Oxazepam Temazepam

MOA for benzodiazepines

Increase the FREQUENCY of GABA-mediated chloride ion channel opening

Benzodiazepine with useful relaxant effects in skeletal muscle spasticity of central origin

Diazepam

Benzodiazepine that has efficacy against absence seizures and in anxiety states, such as agoraphobia

Clonazepam

Benzodiazepines that are the most effective in the treatment of panic disorder

Alprazolam | Clonazepam

Benzodiazepine that is used for anesthesia

Midazolam

DOC for status epilepticus

Diazepam

Longer acting benzodiazepines used in the management of withdrawal states of alcohol and other drugs

Chlordiazepoxide [LIBRIUM] | Diazepam

Agents having active metabolites, long half lives, and a high incidence of adverse effects

Chlordiazepoxide Clorazepate Diazepam Flurazepam

Barbiturates may precipitate this hematologic condition

Acute intermittent porphyria

Barbiturates decrease the effectiveness of many other drugs via this pharmacokinetics property

Liver enzyme INDUCTION

Barbiturates MOA

Increase the DURATION of GABA-mediated chloride ion channels

Barbiturate used for the induction of anesthesia

Thiopental

Important drug interaction with chloral hydrate

May displace coumadin from plasma proteins

Site of action for zaleplon and zolpidem

Benzodiazepine receptor BZ1 (although are not considered benzodiazepines)

Drugs with good hypnotic activity with less CNS SE than most benzodiazepines

Zolpidem | Zaleplon

Agent that is a partial agonist for the 5-HT1A receptor

Buspirone

Drug of choice for generalized anxiety disorder, NOT effective in acute anxiety

Buspirone

Agents with zero-order kinetics

``` Warfarin, Phenytoin Ethanol Aspirin Theophylline Tolbutamide ``` "WPEATT your answer, I got nothing (0)."

Rate limiting step of alcohol metabolism

Aldehyde dehydrogenase

Enzyme that metabolizes acetaldehyde to acetate

Aldehyde dehydrogenase

Agents that inhibit aldehyde dehydrogenase

Disulfiram Metronidazole Cephalosporins Sulfonylureas

Agent used in the treatment of alcoholism, if alcohol is consumed concurrently, acetaldehyde builds up and results in nausea, headache, flushing, and hypotension

Disulfiram [ANTABUSE]

Agent that is teratogen and causes a fetal syndrome

Alcohol

Agent that competes for alcohol dehydrogenase in the case of methanol overdose

Ethanol

Drug that inhibits alcohol dehydrogenase and is used in ethylene glycol exposure

Fomepizole

Most frequent route of metabolism

Hepatic enzymes

Mechanisms of action for Phenytoin, Carbamazepine, Lamotrigine

Sodium blockade

MOA for benzodiazepines and barbiturates

GABA-related targets

MOA for Ethosuximide

Calcium channels

MOA for Valproic acid at high doses

Affect calcium, potassium, and sodium channels

DOC for febrile seizures

Phenobarbital

Drugs of choice for status epilepticus

IV Diazepam/Lorazepam followed by Phenytoin

Drugs that can be used for infantile spasms

Corticosteroids

Anti-seizure drugs used also for bipolar affective disorder (BAD)

Carbamazepine [TEGRETOL] Gabapentin [NEURONTIN] Phenytoin [DILANTIN] and Valproic acid [DEPAKOTE]

Anti-seizure drugs used also for Trigeminal neuralgia

Carbamazepine

Anti-seizure agent that exhibits non-linear metabolism, highly protein bound, causes fetal hydantoin syndrome, and stimulates hepatic metabolism

Phenytoin

Anti-seizure agent that induces formation of liver drug-metabolism enzymes, is teratogenic and can cause craniofacial anomalies and spina bifida

Carbamazepine

Agent that inhibits hepatic metabolism, is hepatotoxic and teratogen that can cause neural tube defects and gastrointestinal distress

Valproic acid

Laboratory value required to be monitored for patients on valproic acid

Serum ammonia and LFT's

SE for Lamotrigine

Stevens-Johnson syndrome

SE for Felbamate

Aplastic anemia | Acute hepatic failure

Anti-seizure medication also used in the prevention of migraines

Valproic acid

Carbamazepine may cause

Agranulocytosis

Anti-seizure drugs used as alternative drugs for mood stabilization

Carbamazepine Gabapentin Lamotrigine Valproic acid

MOA of general anesthetics

Unclear, thought to increase the threshold for firing of CNS neurons

Inhaled anesthetic with a low blood/gas partition coefficient

Nitrous oxide

Inversely related to potency of anesthetics

Minimum alveolar anesthetic concentration (MAC)

Inhaled anesthetics metabolized by liver enzymes which has a major role in the toxicity of these agents

Halothane and methoxyflurane

Most inhaled anesthetics SE

Decrease arterial blood pressure

Inhaled anesthetics are myocardial depressants

Enflurane and halothane

Inhaled anesthetic causes peripheral vasodilation

Isoflurane

Inhaled anesthetic that may sensitize the myocardium to arrhythmogenic effects of catecholamines and has produced hepatitis

Halothane

Inhaled anesthetics, less likely to lower blood pressure than other agents, and has the smallest effect on respiration

Nitrous oxide

Fluoride released by metabolism of this inhaled anesthetic may cause renal insufficiency

Methoxyflurane

Prolonged exposure to this inhaled anesthetic may lead to megaloblastic anemia

Nitrous oxide

Pungent inhaled anesthetic which leads to high incidence of coughing and vasospasm

Desflurane

IV barbiturate used as a pre-op anesthetic

Thiopental

Benzodiazepine used adjunctively in anesthesia

Midazolam

This produces "dissociative anesthesia", is a cardiovascular stimulant which may increases intracranial pressure, and hallucinations occur during recovery

Ketamine

State of analgesia and amnesia produced when fentanyl is used with droperidol and nitrous oxide

Neuroleptanesthesia

Produces both rapid anesthesia and recovery, has antiemetic activity and commonly used for outpatient surgery, may cause marked hypotension (Not meant for home use by pop stars)

Propofol

MOA of local anesthetics (LA's)

Block voltage-dependent sodium channels

This may enhance activity of local anesthetics

Hyperkalemia

This may antagonize activity of local anesthetics

Hypercalcemia

Almost all local anesthetics have this property and sometimes require the administration of vasoconstrictors (ex. Epinephrine) to prolong activity

Vasodilation

Local anesthetic with vasoconstrictive property, favored for head, neck, and pharyngeal surgery

Cocaine

Longer acting local anesthetics which are less dependent on vasoconstrictors

Tetracaine | Bupivacaine

These Local Anesthetics (LA's) have surface activity

Cocaine | Benzocaine

Most important toxic effects of most local anesthetics

CNS toxicity

Commonly abused LA which has cardiovascular toxicity including severe hypertension with cerebral hemorrhage, cardiac arrhythmias, and myocardial infarction

Cocaine

LA causing methemoglobinemia

Prilocaine

Structurally related to acetylcholine, used to produce muscle paralysis in order to facilitate surgery or artifical ventilation. Full doses lead to respiratory paralysis and require ventilation

Neuromuscular blocking drugs

These drugs strongly potentiate and prolong effect of neuromuscular blockade (NMB)

Inhaled anesthetics (esp. Isoflurane) Aminoglycosides Antiarrhythmics

These prevent the action of Ach at the skeletal muscle endplate to produce a "surmountable blockade," effect is reversed by cholinesterase inhibitors (ex. neostigmine or pyridostigmine)

Nondepolarizing type antagonists

Agent with long duration of action and is sost likely to cause histamine release

Tubocurarine

Non-depolarizing antagonist has short duration

Mivacurium

Agent can blocking muscarinic receptors

Pancuronium

Agent undergoing Hofmann elimination (breaking down spontaneously)

Atracurium

One depolarizing blocker that causes continuous depolarization and results in muscle relaxation and paralysis, causes muscle pain postoperatively and myoglobinuria may occur

Succinylcholine

During Phase I these agents worsen the paralysis by succinylcholine, but during phase II they reverse the blockade produced by succinylcholine

Cholinesterase inhibitors

Agents acting in the CNS or in the skeletal muscle, used to reduce abnormally elevated tone caused by neurologic or muscle end plate disease

Spasmolytic drugs

Facilitates GABA presynaptic inhibition

Diazepam

GABA agonist in the spinal cord

Baclofen

Similar to clonidine and may cause hypotension

Tizanidine

Agent used for acute muscle spasm

Cyclobenzaprine

Agent used in drug therapy of Parkinson's instead of Dopamine which has low bioavailability and does not cross the BBB

L-dopa

This is combined with L-dopa, inhibits DOPA decarboxylase (active only peripherally) which allows lower effective doses of L-dopa and allows for fewer SE's (GI distress, postural hypotension, and dyskinesias)

Carbidopa

Clinical response that may fluctuate in tx of Parkinson's dx

On-off-phenomenon

Anti-Parkinson's drug which increases intraocular pressure and is contraindicated in closed angle glaucoma

Levodopa

Ergot alkaloid that is a partial agonist at D2 receptors in the brain, used for patients who are refractory or cannot tolerate levodopa, causes erythromelalgia

Bromocriptine

Non ergot agents used as first-line therapy in the initial management of Parkinson's

Pramipexole [MIRAPEX] | Ropinirole [REQUIP]

Enhances dopaminergic neurotransmission SE's include CNS excitation, acute toxic psychosis and livedo reticularis

Amantadine

Inhibitor of MAO type B which metabolizes dopamine, used adjunct to levodopa or as sole agent in newly diagnosed pt's

Selegiline

Inhibitors of catechol-O-methyltransferase (COMT), used as adjuncts in Parkinson's dx and cause acute hepatic failure (monitor LFT's)

Entacapone | Tolcapone

Agent decreases the excitatory actions of cholinergic neurons. May improve tremor and rigidity but have LITTLE effect on bradykinesia. Atropine-like side effects

Benztropine

Agent effective in physiologic and essential tremor

Propranolol

Agents used in Huntington's Disease

Tetrabenazine (amine depleting drug | Haloperidol (antipsychotic)

Agents used in Tourette's dx

Haloperidol | Pimozide

Chelating agent used in Wilson's disease

Penicillamine

Extrapyramidal dysfunction is more common with these agents, which block this subtype of dopamine receptor

Older antipsychotic agents | D2 receptors

Antipsychotics that reduce positive symptoms only

Older antipsychotics

Newer atypical antipsychotics that also improve some of the negative symptoms and help acute agitation

Olanzapine | Aripiprazole

Atypical antipsychotic causing high prolactin levels

Risperidone

Newer atypical antipsychotic used for bipolar disorder, known to cause weight gain, and adversely affect diabetes

Olanzapine

Agent more frequently associated with extrapyramidal side effects that can be treated with benzodiazepine, diphenhydramine or muscarinic blocker

Haloperidol

Drug used in neuroleptic malignant syndrome

Dantrolene

Agents may exacerbate tardive dyskinesias (may be irreversible and there is no treatment)

Muscarinic blockers

Antipsychotic having the weakest autonomic effects

Haloperidol

Only phenothiazine not exerting antiemetic effects, can cause visual impairment due to retinal deposits, and high doses have been associated with ventricular arrhythmias

Thioridazine

Anti-psychotics available in depot preparation

Fluphenazine | Haloperidol

Drugs that have reduced seizure threshold

Low-potency typical antipsychotics | Clozapine

Orthostatic hypotension and QT prolongation

Low potency and risperidone

Increased risk of developing cataracts

Quetiapine

Major route of elimination for Lithium

Kidneys

Drug increases the renal clearance hence decreases levels of lithium

Theophylline

Lithium is associated with this congenital defect and is contraindicated when?

Cardiac anomalies and is contraindicated in pregnancy or lactation

Example of three antidepressants that are indicated for obsessive compulsive disorder

Clomipramine [ANAFRANIL] Fluoxetine [PAXIL] Fluvoxamine [LUVOX]

Neurotransmitters affected by the action of antidepressants

Norepinephrine | Serotonin

Usual time needed for full effect of antidepressant therapy

2 to 3 weeks

Population group especially sensitive to side effects of antidepressants

Elderly patients

All antidepressants have roughly the same efficacy in treating depression, agents are chosen based on these criterion

Side-effect profile and prior pt response

Well-tolerated first-line antidepressants

SSRI's [e.g. CELEXA, LEXAPRO, PAXIL, PROZAC] Bupropion [WELLBUTRIN] Venlafaxine [EFFEXOR XR]

Most useful in patients with significant anxiety, phobic features, hypochondriasis, and resistant depression

Monamine oxidase inhibitors

Condition will result from in combination of MAOI with tyramine containing foods (ex. wine, cheese, and pickled meats)

Hypertensive crisis

MAOI should not be administered with SSRI's or potent TCA's due to development of this condition

Serotonin syndrome

Sedation is a common side effect of these drugs, they lower seizure threshold, uses include BAD, acute panic attacks, phobias, enuresis, and chronic pain and their overdose can be deadly

Tricyclic antidepressants (TCA)

Three C's associated with TCA toxicity

Cardiac problems (arrhythmias and wide QRS) Convulsions Coma

Agents having higher sedation and antimuscarinic effects than other TCA's

Tertiary amines

TCA used in chronic pain, a hypnotic, and has marked antimuscarinic effects

Amitriptyline

TCA with greatest sedation of this group, and marked antimuscarinic effects, used for sleep

Doxepin

TCA used in obsessive compulsive disorder (OCD), most significant of TCA's for risk of seizure, weight gain, and neuropsychiatric signs and symptoms

Clomipramine

Secondary amines that have less sedation and more excitation effect

Nortriptyline | Desipramine

Antidepressant associated with neuroleptic malignant syndrome

Amoxapine

Antidepressant associated with seizures and cardiotoxicity

Maprotiline

Antidepressant having stimulant effects similar to SSRI's and can increase blood pressure

Venlafaxine

Antidepressant inhibiting norepinephrine, serotonin, and dopamine reuptake

Venlafaxine

Antidepressant also used for sleep that causes priapism

Trazodone

Antidepressant which is inhibitor of CYP450 enzymes and may be associated with hepatic failure

Nefazodone

Antidepressant with MOA as alpha 2 antagonist, has effects on both 5-HT and NE, blocks histamine receptors, and is sedating

Mirtazapine

SE of mirtazapine

Liver toxicity | Increased serum cholesterol

Except for these agents all SSRI have significant inhibition of CytP450 enzymes

Citalopram | Escitalopram (metabolite of Citalopram)

SSRI with long T1/2 and can be administered once weekly for maintenance, not acute tx

Fluoxetine

SSRI indicated for premenstrual dysphoric disorder

Fluoxetine (Sarafem)

Some of SSRIs' therapeutic effects beside depression

``` Panic attacks PMDD (premenstrual dysphoric disorder) Social phobias OCD Bulimia nervosa ``` "PP don't SOB"

SSRI's less likely to cause a withdrawal syndrome

Fluoxetine

Inhibit synaptic activity of primary afferents and spinal cord pain transmission neurons

Ascending pathways

Activation of these receptors open K+ ion channels to cause membrane hyperpolarization

Postsynaptic Mu receptors

All opioids except this agent (which has a muscarinic blocking action) cause pupillary constriction

Meperidine

SE of these drugs include dependence, withdrawal syndrome, sedation, euphoria, respiratory depression nausea and vomiting, constipation, biliary spasm, increased ureteral and bladder tone, and reduction in uterine tone

Opioid Analgesics

Strong opioid agonists

Fentanyl Morphine Meperidine Methadone

Opioids used in anesthesia

Fentanyl | Morphine

Use of this opioid with MAOI can lead to hyperpyrexic coma, and with SSRI's can lead to serotonin syndrome

Meperidine

Weak opioid agonist, poor analgesic, its overdose can cause severe toxicity including respiratory depression, circulatory collapse, pulmonary edema, and seizures

Propoxyphene

Partial opioid agonist, considered a strong analgesic, has a long duration of action and is resistant to naloxone reversal

Buprenorphine

These agents are used as antitussive

Codeine | Dextromethorphan

These agents are used as antidiarrheal

Diphenoxylate [LOMOTIL] | Loperamide [IMMODIUM]

Inhalant anesthetics

Nitric oxide (NO) Chloroform Diethyl ether "Anesthetics will have 'NOC'D you out"

Toxic to the liver, kidney, lungs, bone marrow, peripheral nerves, and cause brain damage in animals, sudden death has occurred following inhalation

Fluorocarbons and Industrial solvents

Cause dizziness, tachycardia, hypotension, and flushing

Organic nitrites

Causes acne, premature closure of epiphyses, masculinization in females, hepatic dysfunction, MI, and increases in libido and aggression

Steroids

Most commonly abused drugs in health care professionals

``` Heroin Morphine Meperidine Fentanyl Oxycodone ``` "HMM, Feeling Overwhelmed?"

This route is associated with rapid tolerance and psychologic dependence

IV administration

Lacrimation, rhinorrhea, yawning, sweating, weakness, gooseflesh, nausea, and vomiting, tremor, muscle jerks, and hyperpnea are signs of this syndrome

Abstinence syndrome

Treatment for opioid addiction

Methadone, followed by slow dose reduction

Sedative-Hypnotics action

Reduce inhibition, suppress anxiety, and produce relaxation

Additive effects when Sedative-Hypnotics used in combination with these agents

CNS depressants

Common mechanism by which overdose result in death

Depression of medullary and cardiovascular centers

The most important sign of withdrawal syndrome

Excessive CNS stimulation (seizures)

Treatment of withdrawal syndrome involves

Long-acting sedative-hypnotic Gradual reduction of dose Clonidine Propranolol

Withdrawal from this drug causes lethargy, irritability, and headache

Caffeine

W/D from this drug causes anxiety and mental discomfort

Nicotine

Chronic high dose abuse of nicotine leads to

``` Seizures Hyperreflexia Agitation Restlessness --> Tachycardia, Hyperthermia Psychotic state ``` "Smoking just isn't SHARP"

Tolerance is marked and abstinence syndrome occurs with use of these drugs

Amphetamines

Amphetamine agents

Methamphetamine Dextroamphetamines "MDs need to boost their energy"

These agents are congeners (closely related/same class) of Amphetamine

DOM (dimethoxy-4-methylamphetamine) aka STP "Serenity, Tranquility, and Peace" MDA (3,4-Methylenedioxyamphetamine) MDMA (3,4-methylenedioxyamphetamine) aka "Ecstasy"

Overdoses of this agent with powerful vasoconstrictive action may result in fatalities from arrhythmias, seizures, respiratory depression, or severe HTN (MI and stroke)

Cocaine "super-speed"

Most dangerous of the currently popular hallucinogenic drugs, OD leads to nystagmus, marked hypertension, and seizures, presence of both horizontal and vertical nystagmus is pathognomonic

PCP

Removal of PCP may be aided

Urinary acidification and activated charcoal or continual nasogastric suction

Muscarinic that is very lipid soluble and used in glaucoma

Pilocarpine

Muscarinic used to treat dry mouth in Sjögren's syndrome

Pilocarpine | Cevimeline

Indirect-Acting ACh Agonist, alcohol, short DOA and used in diagnosis of myasthenia gravis

Edrophonium

Carbamate with intermediate action and used as off-label for postoperative paralytic ileus and urinary retention

Neostigmine

Treatment of atropine overdose and glaucoma (because lipid soluable). Enters the CNS rapidly and has a stimulant effect, which may lead to convulsions

Physostigmine

Treatment of myasthenia gravis and sometimes used prophylactically for organophosphate poisoning in chemical warfare

Pyridostigmine

Antiglaucoma organophosphate, indicated but not used much clinically anymore due to long duration of action

Echothiophate

Insecticide organophosphates

Malathion | Parathion

The most important cause of acute deaths in cholinesterase inhibitor toxicity

Respiratory failure

Treatment of muscarinic symptoms in organophosphate overdose

Atropine

This agent competes for phosphorylated cholinesterase enzyme and regenerates enzyme if organophosphate-enzymes complex has not "aged"

Pralidoxime (2-PAM)

Prototypical drug is atropine

Nonselective Muscarinic Antagonists

Reduce transient hyper GI motility

Dicyclomine | Methscopolamine

Cystitis, postoperative bladder spasms, or incontinence

Oxybutynin [DITROPAN] | Dicyclomine [BENTYL]

Toxicity of anticholinergics

Anti-DUMBBELSS

Another pneumonic for anticholinergic toxicity

``` Dry as a bone Red as a beet Mad as a hatter Hot as a hare Blind as a bat ```

Atropine fever is the most dangerous effect and can be lethal in this population group

Infants

Contraindications to use of atropine

Infants Closed angle glaucoma Prostatic hypertrophy

Ganglion blockers that were indicated (but not anymore) for severe hypertension

Hexamethonium | Ttrimethaphan

Reversal of blockade by neuromuscular blockers

Cholinesterase inhibitors

Tubocurarine is the prototype, pancuronium, atracurium, vecuronium are newer short acting agent, produce competitive block at end plate nicotinic receptor, causing flaccid paralysis

Nondepolarizing Neuromuscular Blockers

Only member of depolarizing neuromuscular blocker, causes fasciculation during induction and muscle pain after use

Succinylcholine

This is the drug of choice for anaphylactic shock

Epinephrine

Phenylisopropylamines that are used legitimately and abused for narcolepsy, attention deficit disorder, and weight reduction

Amphetamines

Alpha agonist used to produce mydriasis and reduce conjunctival itching and congestion caused by irritation or allergy, it does not cause cycloplegia

Phenylephrine

Epinephrine and dipivefrin are used for

Glaucoma

Newer alpha 2 agonist (apraclonidine and brimonidine) treat glaucoma

Reduce aqueous synthesis

Short acting Beta 2 agonists that is drug of choice in treatment of acute asthma but not recommended for prophylaxis

Albuterol

Longer acting Beta 2 agonists is recommended for prophylaxis of asthma

Salmeterol

These agents increase blood flow and may be beneficial in treatment of acute heart failure and some types of shock

Beta1 agonists

Shock due to septicemia or myocardial infarction is made worse by

Increasing afterload and tissue perfusion declines

Often mixed with local anesthetic to

Reduce the loss from area of injection

Chronic orthostatic hypotension can be treated with

Midodrine

Beta 2 agonist used to suppress premature labor, but cardiac stimulatory effects may be hazardous to mother and fetus

Terbutaline

Long acting sympathomimetic, sometimes used to improve urinary continence in children and elderly with enuresis

Ephedrine

Beta 1 agonist toxicity

Sinus tachycardia | Arrhythmias

Beta 2 agonist toxicity

Skeletal muscle tremor

The selective agents lose their selectivity at

high doses

Nonselective alpha-blocking drug, long acting and irreversible, and used to treat pheochromocytoma. Blocks 5-HT, so occasionaly used for carcinoid tumor. Blocks H1 and used in mastocytosis

Phenoxybenzamine

Nonselective alpha-blocking drug, short acting and reversible, used for rebound HTN from rapid clonidine withdrawal, and Raynaud's phenomena

Phentolamine

Selective Alpha 2 blocker used for impotence (controversial effectiveness)

Yohimbine

Combined alpha and beta blocking agents that may have application in treatment of CHF

Labetalol | Carvedilol

Beta blockers partial agonist activity (intrinsic sympathomimetic activity) cause some bronchodilation and may have an advantage in treating patients with asthma

Pindolol | Acebutolol

This parenteral beta blocker is a short acting

Esmolol

This beta blocker is the longest acting

Nadolol

These beta blockers are less lipid soluble

Acebutolol | Atenolol

This beta blocker is highly lipid soluble and may account for side effects such as nightmares

Propranolol

Clinical uses of these agents include treatment of HTN, angina, arrhythmias, and chronic CHF

Beta blockers

Toxicity of these agents include bradycardia, AV blockade, exacerbation of acute CHF, signs of hypoglycemia may be masked (tachycardia, tremor, and anxiety)

Beta blockers

Cholinomimetics that increase outflow, open trabecular meshwork, and cause ciliary muscle contraction

Pilocarpine Carbachol Physostigmine

Nonselective alpha agonists that decrease aqueous production and increase aqueous outflow

Epinephrin | Dipivefrin

Selective alpha agonists that decreases aqueous secretion

Apraclonidine | Brimonidine [ALPHAGAN-P]

This diuretic decreases aqueous secretion due to lack of HCO3- ion. Causes drowsiness and paresthesias, alkalinization of the urine may precipitate calcium salts, hypokalemia, acidosis

Acetazolamide

These agents cause increased aqueous outflow

Prostaglandin PGF2a | Latanoprost, travoprost, unoprostone

Inhibit angiotensin-converting enzyme (ACE)

ACE inhibitors

Block L-type calcium channel

Calcium channel blockers

CCB with predominate effect on arteriole dilation

Nifedipine

Beta-blockers should be used cautiously in which disease states?

Asthma (bronchospastic effects) Diabetes (block signs of hypoglycemia) Peripheral vascular disease

Non-selective Beta-blocker also used for migraine prophylaxis

Propranolol

Non-selective Alpha1blockers use to treat pheochromocytoma

Phenoxybenzamine

For rebound HTN from rapid clonidine withdrawal

Phentolamine

Presynaptic Alpha 2 agonist used in HTN

Clonidine | Methyldopa

SE of methyldopa

Positive Comb's test | Depression

SE of clonidine

Dry mouth Rebound HTN Sedation "DRS. talk so much it's like they CLONed themselves"

Direct vasodilator of arteriolar smooth muscle

Hydralazine

Arterial vasodilator that works by opening K+ channels

Minoxidil

SE of minoxidil

Hypertrichosis

IV Drug used Hypertensive Crisis

Nitroprusside

Nitroprusside vasodilates

Arteries and veins

Toxicity caused by nitroprusside | Treatment of toxicity?

Cyanide toxicity | Treated with sodium thiosulfate

Carbonic anhydrase inhibitor

Acetazolamide

Mechanism of action of loop diuretics

inhibits Na+/K+/2Cl- cotransporter

Diuretics used in hypertensive patients with renal failure

Loop diuretics | Furosemide, Ethacrynic acid, Bumetanide

Aminoglycosides used with loop diuretics potentiate this adverse effect

Ototoxicity

Mechanism of action of thiazide diuretics

Inhibit Na+/Cl- cotransport

Diuretic used as first line for treatment of hypertension

Thiazides

Class of drugs that may cause cross-sensitivity with thiazide diuretics

Sulfonamides

Mechanism of action of spironolactone

Inhibit mineralocorticoid receptor and inhibit Na/K-ATPase and ENaC synthesis

ADH agonist used for central diabetes insipidus

Desmopressin (DDAVP)

Agents used for SIADH

Tolvaptan | Conivaptan

An early generation tetracyclin that may be used for chronic persistant SIADH

Demeclocycline

Side effect of demeclocycline

Bone marrow and teeth discoloration for children under 8 years of age

Important side effects of Quinidine

Thrombocytopenic purpura | CINCHONISM

Major drug interaction with Quinidine

Increases concentration of Digoxin

DOC for digoxin induced arrhythmias

Phenytoin

SE of phenytoin

Gingival hyperplasia

Class of anti-arrhythmics that has a pro-arrhythmic effect (CAST trial), therefore are used as last line agents

``` Class IC (Flecainide, Propafenone, Moricizine) ```

Class II antiarrhythmics are

B-blockers

Antiarrhythmic that exhibits Class II and III properties

Sotalol

Side effect of sotalol

prolongs QT and PR interval

Used intravenously for acute arrhythmias during surgery

Esmolol

Anti-arrhythmics that decrease mortality

B-blockers

MOA of class III antiarrhythmics

Potassium channel blockers

Class III antiarrhythmic that exhibits properties of all 4 classes

Amiodarone

Specific pharmacokinetic characteristic of amiodarone

Prolonged half-life, up to six weeks

Antiarrhythmic effective in most types of arrhythmia

Amiodarone

SE of Amiodarone

``` Thyroid dysfunction Photosensitivity Skin (blue smurf syndrome) Corneal deposits Liver damage Pulmonary fibrosis ``` "TP SCaLP"

MOA of class IV antiarrhythmics

Calcium channel blockers

Agent to treat torsades de pointes

Magnesium sulfate

Drug used supraventricular arrhythmias

Digoxin

Unstarred - Deck 1 Flashcards

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