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292 Cards in this Set

  • Front
  • Back
Bethanechol
Direct Acting Cholinergic Agonist

Postoperative and neurogenic ileus and urinary retention

Activates Bowel and Bladder smooth muscle

Beth Anne call me to activate your bowels and bladder
Carbachol
Direct Acting Cholinergic Agonist

Glaucoma, Pupillary Contraction, Release of intraocular pressure
Pilocarpine
Direct Acting Cholinergic Agonist

Stimulates Sweat, Tears, and Saliva

Contracts ciliary muscle of the eye (open angle), pupillary schincter (closed angle)

Resistant to AChE

PILE on the sweat and tears
Methacholine
Direct Acting Cholinergic Agonist

Challenge test for diagnosis of asthma

Stimulates muscarinic receptors in airway when inhaled
Neostigmine
Indirect Acting Cholinergic Agonist

Postoperative and neurogenic ileus and urinary retention

Myathenia Gravis

Reversal of NMJ blockade post-operative

Increases endogenous ACh

No CNS penetration

NEO CNS = NO CNS
Pyridostigmine
Indirect Acting Cholinergic Agonist

Myasthenia Gravis (long-acting)

Increases endogenous ACh

No CNS
Edrophonium
Indirect Acting Cholinergic Agonist

Diagnosis of Myasthenia Gravis (very short-acting)

Increases endogenous ACh
Physostigmine
Glaucoma

Atropine overdose

Increases endogenous ACh

PHYS is for EYES
Ectothiophate
Glaucoma

Increases endogenous ACh
Atropine
Muscarinic Antagonist

Eye

Produce mydriasis and cycloplegia
Homatropine
Muscarinic Antagonist

Eye

Produce mydriasis and cycloplegia
Tropicamide
Muscarinic Antagonist

Eye

Produce mydriasis and cycloplegia
Benztropine
Muscarinic Antagonist

CNS

Parkinson's Disease

PARK my BENZ
Scopolamine
Muscarinic Antagonist

CNS

Motion Sickness
Ipratropium
Muscarinic Antagonist

Respiratory

Asthma, COPD

I PRAY I can breathe soon
Oxybutynin
Muscarinic Antagonist

Genitourinary

Reduce urgency in mild Cystitis
Glycopyrrolate
Muscarinic Antagonist

Genitourinary

Reduce urgency in mild Cystitis
Methscopolamine
Muscarinic Antagonist

Gastrointestinal

Peptic Ulcer treatment
Pirenzepine
Muscarinic Antagonist

Gastrointestinal

Peptic Ulcer treatment
Propantheline
Muscarinic Antagonist

Gastrointestinal

Peptic Ulcer treatment
Hexamethonium
Nicotinic Antagonist

Ganglionic blocker

Used in experiments to prevent vagal reflex responses to changes in blood pressure

Prevents Reflex Bradycardia caused by NE

Put a HEX on smokers (nicotine)

----------------------------------------------
Severe Orthostatic Hypertension

Blurred Vision

Constipation

Sexual Dysfunction
Epinephrine
Alpha 1 and 2
Beta 1 and 2

Low dose selective for Beta 1 (Blow)

Anaphylaxis

Glaucoma (open angle)

Asthma

Hypotension
Norepinephrine
Alpha 1 and 2

Hypotension

(but DECREASES renal perfusion)
Isoproterenol
Beta 1 and 2

AV Block
Dopamine
D1 and D2 > Beta > Alpha

Inotropic and Chronotropic

Heart Failure

Shock
(INCREASES renal perfusion)
Dobutamine
Beta 1 > Beta 2

Inotropic (NOT Chronotropic)

Heart Failure

Shock

Cardiac Stress Testing
Phenylephrine
Alpha 1 > Alpha 2

Pupillary Dilation

Vasoconstriction

Nasal Decongestion
Albuterol
Beta 2 > Beta 1

Acute Asthma
Terbutaline
Beta 2 > Beta 1

Reduces Premature Uterine Contractions
Ritrodine
Beta 2

Reduces Premature Uterine Contractions
Ampthetamine
Releases stores catecholamines

Narcolepsy

Obesity

Attention Deficit Disorder (ADD)
Ephedrine
Releases stored catecholamines

Nasal Decongestion

Urinary Incontinence

Hypotension
Cocaine
Uptake Inhibitor

Vasoconstriction

Local Anesthesia
Clonidine
Centrally acting Alpha 2 Agonist

DECREASES Central adrenergic outflow

Hypertension
(NO decrease in renal perfusion)

------------------------------------------------
Dry Mouth

Sedation

Severe Rebound Hypertension
ά-Methyldopa
Centrally acting Alpha 2 Agonist

DECREASES Central adregergic outflow

Hypertension
(NO decrease in renal perfusion)

---------------------------------------------
Sedation

+ Coomb's test
Selective Beta 2 Agonists
MAST:

Metaproterenol

Albuterol

Salmeterol

Terbutaline
Phenoxybenzamine
Non-Selective Alpha Blocker

(IRREVERSIBLE)

Pheochromocytoma (before removing tumor)

---------------------------------------------
Orthostatic Hypotension

Reflex Tachycardia
Phentolamine
Non-Selective Alpha Blocker

(REVERSIBLE)

Pheochromocytoma (before removing tumor)

----------------------------------------------------
Orthostatic Hypotension

Reflex Tachycardia
Prazosin
Alpha-1 Selective Blocker

Hypertension

Urinary Retention in BPH

--------------------------------------------
1st dose Orthostatic Hypotension

Dizziness

Headache
Terazosin
Alpha-1 Selective Blocker

Hypertension

Urinary Retention in BPH

--------------------------------------------
1st dose Orthostatic Hypotension

Dizziness

Headache
Doxazosin
Alpha-1 Selective Blocker

Hypertension

Urinary Retention in BPH

--------------------------------------------
1st dose Orthostatic Hypotension

Dizziness

Headache
Mirtazapine
Alpha-2 Selective Blocker

Depression

---------------------------------------------------
Sedation

Increase Serum Cholesterol

Increase Appetite
Non-Selective Beta Blockers
Propanolol

Pindolol

Nadolol

Timolol

Labetalol
Beta-1 Selective Blockers
Acebutolol (partial agonist)

Betaxolol

Esmolol (short acting)

Atenolol

Metoprolol

A BEAM of beta-1 blockers
Non-Selective Alpha and Beta Blockers
Carvedilol

Labetolol
Partial Beta Agonists
Pindolol

Acebutolol
Sulfa Drugs
Celecoxib

Furosemide

Probenecid

Thiazides

TMP-SMX

Sulfasalazine

Sulfonylureas

Sumatriptan
Hydrochlorothiazide
Diuretic

-----------------------------------------------
Hypokalemia

Mild Hyperlipidemia

Hyperuricemia

Lassitude

Hypercalcemia

Hyperglycemia
Loop Diuretics
Diuretic

---------------------------------------------------
K+ Wasting

Metabolic Alkalosis

Hypotension

Ototoxicity
Reserpine
Sympatholytic

-----------------------------------------------
Sedation

Depression

Nasal stuffiness

Diarrhea
Guanethidine
Sympatholytic

-----------------------------------------------
Orthostatic and Exercise Hypotension

Sexual Dysfunction

Diarrhea
Hydralazine
Vasodilator

Increases cGMP -> smooth muscle relaxation

Vasodilates arterioles > veins

Afterload reduction

Severe Hypertension, CHF

1st line in pregnancy, with Methyldopa
------------------------------------------
Nausea

Headache

Lupus-like Syndrome

Reflex Tachycardia (use w/ beta blocker to block) (contraindicated in angina/CAD)

Angina

Water / Salt Retention (use w/ diuretic to block)
Minoxidil
Vasodilator

K+ Channel opener -> Hyperpolarizes and relaxes vascular smooth muscle

Severe Hypertension
------------------------------------------
Hypertrichosis

Pericardial Effusion

Reflex Tachycardia (use w/ beta blocker to block)

Angina

Salt Retention (use w/ diuretic to block)
Nifedipine
Vasodilator

Block voltage-dependent L-type Ca2+ channels of cardiac and smooth muscle and so reduce contractility

Vascular smooth muscle: Nifedipine > Diltiazem > Verapamil

Heart: Verapamil > Diltiazem > Nifedipine

Hypertension

Angina

Prinzmetal's Angina

Raynaud's Phenomenon
------------------------------------------------
Cardiac Depression

Dizziness

Flushing

Nausea

Edema

Constipation
Verapamil
Vasodilator

Block voltage-dependent L-type Ca2+ channels of cardiac and smooth muscle and so reduce contractility

Vascular smooth muscle: Nifedipine > Diltiazem > Verapamil

Heart: Verapamil > Diltiazem > Nifedipine

Arrhythmias

Hypertension

Angina

Prinzmetal's Angina

Raynaud's Phenomenon
------------------------------------------------
Cardiac Depression

Dizziness

Flushing

Nausea

Edema

Constipation
Diazoxide
Vasodilator

K+ Channel opener -> hyperpolarizes and relaxes vascular smooth muscle

Malignant Hypertension

------------------------------------------
Hyperglycemia (reduces insulin release, hypotension)
Captopril
ACE Inhibitor

--------------------------------------------
Hyperkalemia

Cough

Angioedema

Taste Changes

Hypotension

Pregnancy Problem (fetal renal problems)

Rash

Renin
Enalapril
ACE Inhibitor

-----------------------------------------------
Hyperkalemia

Cough

Angioedema

Taste Changes

Hypotension

Pregnancy Problem (fetal renal problems)

Rash

Renin
Fosinopril
ACE Inhibitor

--------------------------------------------
Hyperkalemia

Cough

Angioedema

Taste Changes

Hypotension

Pregnancy Problem (fetal renal problems)

Rash

Renin
Losartan
Angiotensin II Receptor Blocker (ARB)

--------------------------------------------
Fetal Renal Toxicity

Hyperkalemia
Diltiazem
Vasodilator

Block voltage-dependent L-type Ca2+ channels of cardiac and smooth muscle and so reduce contractility

Vascular smooth muscle: Nifedipine > Diltiazem > Verapamil

Heart: Verapamil > Diltiazem > Nifedipine

Arrhythmias

Hypertension

Angina

Prinzmetal's Angina

Raynaud's Phenomenon
------------------------------------------------
Cardiac Depression

Dizziness

Flushing

Nausea

Edema

Constipation
Nitroglycerin
Vasodilate by releasing NO in smooth muscle, causing increased cGMP and smooth muscle relaxation

veins >> arteries

Decreases preload

Angina

Pulmoary Edema

Aphrodisiac

Erection Enhancer

-----------------------------------------------
Tachycardia

Hypotension

Flushing

Headache

"Monday Disease"
Isosorbide Dinitrate
Vasodilate by releasing NO in smooth muscle, causing increased cGMP and smooth muscle relaxation

veins >> arteries

Decreases preload

Angina

Pulmonary Edema

Aphrodisiac

Erection Enhancer

-----------------------------------------------
Tachycardia

Hypotension

Flushing

Headache

"Monday Disease"
Nitroprusside
Short acting

Increases cGMP via direct release of NO

Malignant Hypertension

------------------------------------------
Cyanide Toxicity (releases CN)
Fenolodpam
Dopamine D1 receptor agonist -> relaxes renal vascular smooth muscle

Malignant Hypertension
Lovastatin
HMG-CoA Reductase Inhibitor
(decreases mevalonate)

Decreases LDL

-----------------------------------------------
Reversible INCREASED LFTs

Rhabdomyolysis
Pravastatin
HMG-CoA Reductase Inhibitor
(decreases mevalonate)

Decreases LDL

-----------------------------------------------
Reversible INCREASES LFTs

Rhabdomyolysis
Simvustatin
HMG-CoA Reductase Inhibitor
(decreases mevalonate)

Decreases LDL

-----------------------------------------------
Reversible INCREASES LFTs

Rhabdomyolysis
Atorvastatin
HMG-CoA Reductase Inhibitor
(decreases mevalonate)

Decreases LDL

-----------------------------------------------
Reversible INCREASES LFTs

Rhabdomyolysis
Rosuvastatin
HMG-CoA Reductase Inhibitor
(decreases mevalonate)

Decreases LDL

-----------------------------------------------
Reversible INCREASES LFTs

Rhabdomyolysis
Niacin
Inhibits lipolysis in adipose tissue

Reduces hepatic VLDL secretion into circulation

Increases HDL

---------------------------------------------
Red, Flushed face
(decrease with aspirin or long-term use)
Cholestyramine
Bile Acid Sequestrant

Prevents intestinal reabsorption of bile acids

Liver must use cholesterol to make

Decreases LDL

------------------------------------------------
Patients hate it

Tastes bad

GI discomfort

Decrease absorption of ADEK

Contraindicated in Gallstones
Colestipol
Bile Acid Sequestrant

Prevents intestinal reabsorption of bile acids

Liver must use cholesterol to make

Decreases LDL

------------------------------------------------
Patients hate it

Tastes bad

GI discomfort

Decrease absorption of ADEK

Contraindicated in Gallstones
Colesevelam
Bile Acid Sequestrant

Prevents intestinal reabsorption of bile acids

Liver must use cholesterol to make

Decreases LDL

------------------------------------------------
Patients hate it

Tastes bad

GI discomfort

Decrease absorption of ADEK

Contraindicated in Gallstones
Ezetimibe
Cholesterol Absorption Blockers

Prevents cholesterol reabsorption at small intestinal brush border

Decreases LDL

-------------------------------------------------
Rare Increased LFTs
Gemfibrozil
Upregulates LPL to increase Triglyceride clearance

Decreases TG

--------------------------------------------------
Myositis

Increases LFTs
Clofibrate
Upregulates LPL to increase Triglyceride clearance

Decreases TG

--------------------------------------------------
Myositis

Increases LFTs
Fenofibrate
Upregulates LPL to increase Triglyceride clearance

Decreases TG

--------------------------------------------------
Myositis

Increases LFTs
Digoxin
Direct inhibition of Na/K ATPase leads to indirect inhibition of Na/Ca exchanger to increase intracellular Ca

CHF

Atrial Fibrillation

-------------------------------------------Blurry Yellow Vision

Arrhythmia

Toxicity increased by hypokalemia

Antidote is K+, Lidocaine, Digi-bind Fab fragments, Mg2+
Quinidine
Class IA Antiarrhythmic

Na+ channel blocker

Atrial and Ventricular Arrhythmias

Reentrant and Ectopic Supraventricular and Ventricular Arrhythmias

------------------------------------------
Cinchonism (headache, tinnitus, thrombocytopenia, torsades de pointes
Procainamide
Class IA Antiarrhythmic

Na+ channel blocker

Atrial and Ventricular Arrhythmias

Reentrant and Ectopic Supraventricular and Ventricular Arrhythmias

------------------------------------------------------
Reversible SLE-like Syndrome
Disopyramide
Class IA Antiarrhythmic

Na+ channel blocker

Atrial and Ventricular Arrhythmias

Reentrant and Ectopic Supraventricular and Ventricular Arrhythmias
Lidocaine
Class IB Antiarrhythmic

Na+ channel blocker

Acute Ventricular Arrhythmia

Digitalis-induced Arrhythmia

----------------------------------------
Local Anesthetic

CNS stimulation/depression

Cardiovascular Depression
Mexiletine
Class IB Antiarrhythmic

Na+ channel blocker

Acute Ventricular Arrhythmia

Digitalis-induced Arrhythmia

----------------------------------------
Local Anesthetic

CNS stimulation/depression

Cardiovascular Depression
Tocainide
Class IB Antiarrhythmic

Na+ channel blocker

Acute Ventricular Arrhythmia

Digitalis-induced Arrhythmia

----------------------------------------
Local Anesthetic

CNS stimulation/depression

Cardiovascular Depression
Flecanide
Class IC Antiarrhythmic

Ventricular Tachycardia that progresses to Ventricular Fibrillation

Intractable Supraventricular Tachycardia

Last resort in refractory tachyarrythmias

------------------------------------------
For patients without structural abnormalities

Proarrhythmic, especially post-MI

Prolongs refractory period in AV node
Encainide
Class IC Antiarrhythmic

Ventricular Tachycardia that progresses to Ventricular Fibrillation

Intractable Supraventricular Tachycardia

Last resort in refractory tachyarrythmias

------------------------------------------
For patients without structural abnormalities

Proarrhythmic, especially post-MI

Prolongs refractory period in AV node
Propafenone
Class IC Antiarrhythmic

Ventricular Tachycardia that progresses to Ventricular Fibrillation

Intractable Supraventricular Tachycardia

Last resort in refractory tachyarrythmias

------------------------------------------
For patients without structural abnormalities

Proarrhythmic, especially post-MI

Prolongs refractory period in AV node
Propanolol
Class II Antiarrythmic

Beta-blocker

Ventricular Tachycardia

Supraventricular Tachycardia

Atrial Fibrillation/Flutter

-----------------------------------------
Impotence

Asthma

Bradycardia, AV Block, CHF

Sedation, Sleep disturbance

May mask hypoglycemia
Esmolol
Class II Antiarrythmic

Beta-blocker

Ventricular Tachycardia

Supraventricular Tachycardia

Atrial Fibrillation/Flutter

-----------------------------------------
Impotence

Asthma

Bradycardia, AV Block, CHF

Sedation, Sleep disturbance

May mask hypoglycemia
Metoprolol
Class II Antiarrythmic

Beta-blocker

Ventricular Tachycardia

Supraventricular Tachycardia

Atrial Fibrillation/Flutter

-----------------------------------------
Impotence

Asthma

Bradycardia, AV Block, CHF

Sedation, Sleep disturbance

May mask hypoglycemia

DYSLIPIDEMIA
Atenolol
Class II Antiarrythmic

Beta-blocker

Ventricular Tachycardia

Supraventricular Tachycardia

Atrial Fibrillation/Flutter

-----------------------------------------
Impotence

Asthma

Bradycardia, AV Block, CHF

Sedation, Sleep disturbance

May mask hypoglycemia
Timolol
Class II Antiarrythmic

Beta-blocker

Ventricular Tachycardia

Supraventricular Tachycardia

Atrial Fibrillation/Flutter

-----------------------------------------
Impotence

Asthma

Bradycardia, AV Block, CHF

Sedation, Sleep disturbance

May mask hypoglycemia
Sotalol
Class III Antiarrhythmic

K+ channel blocker

Use when other anti-arrhythmics fail

-----------------------------------------------
Torsades de Pointes

Excessive Beta-block
Ibutilide
Class III Antiarrhythmic

K+ channel blocker

Use when other anti-arrhythmics fail

----------------------------------------------
Torsades de Pointes
Bretylium
Class III Antiarrhythmic

K+ channel blocker

Use when other anti-arrhythmics fail

---------------------------------------------
New arrhythmias

Hypotension
Amiodarone
Class III Antiarrhythmic

K+ channel blocker

Use when other anti-arrhythmics fail

------------------------------------------
Pulmonary Fibrosis

Hepatotoxicity

Hypo/Hyperthyroidism

Corneal deposits

Skin deposits, photodermatitis

Neurologic effects

Check PFTs, LFTs, TFTs
Verapamil
Class IV Antiarrhythmic

Ca2+ channel blockers

Prevent Nodal Arrythmias (SVT)

---------------------------------------------
Constipation

Flushing

Edema

AV Block, CHF, Sinus node depression
Diltiazem
Class IV Antiarrhythmic

Ca2+ channel blockers

Prevent Nodal Arrythmias (SVT)

---------------------------------------------
Constipation

Flushing

Edema

AV Block, CHF, Sinus node depression
Adenosine
Increases K+ out of cells to hyperpolarize them and decreases inward Ca2+ current

Drug of choice in diagnosing/abolishing AV nodal arrhythmias

------------------------------------------Hypotension

Flushing

Chest pain
K+
Depresses ectopic pacemakers in hypokalemia (digoxin toxicity)
Mg2+
Effective in Torsades de Pointes and Digoxin toxicity
Lispro
Insulin

Short-acting

Binds insulin receptor (tyrosine kinase activity)

Type I DM
Type II DM

Life-threatening Hyperkalemia

Stress-induced Hyperglycemia

-------------------------------------------
Hypoglycemia

Hypersensitivity Reaction
Aspart
Insulin

Short-acting

Binds insulin receptor (tyrosine kinase activity)

Type I DM
Type II DM

Life-threatening Hyperkalemia

Stress-induced Hyperglycemia

-------------------------------------------
Hypoglycemia

Hypersensitivity Reaction
Regular Insulin
Insulin

Short-acting

Binds insulin receptor (tyrosine kinase activity)

Type I DM
Type II DM

Life-threatening Hyperkalemia

Stress-induced Hyperglycemia

-------------------------------------------
Hypoglycemia

Hypersensitivity Reaction
NPH
Insulin

Intermediate-acting

Binds insulin receptor (tyrosine kinase activity)

Type I DM
Type II DM

Life-threatening Hyperkalemia

Stress-induced Hyperglycemia

-------------------------------------------
Hypoglycemia

Hypersensitivity Reaction
Glargine
Insulin

Long-acting

Binds insulin receptor (tyrosine kinase activity)

Type I DM
Type II DM

Life-threatening Hyperkalemia

Stress-induced Hyperglycemia

-------------------------------------------
Hypoglycemia

Hypersensitivity Reaction
Detemir
Insulin

Long-acting

Binds insulin receptor (tyrosine kinase activity)

Type I DM
Type II DM

Life-threatening Hyperkalemia

Stress-induced Hyperglycemia

-------------------------------------------
Hypoglycemia

Hypersensitivity Reaction
Tolbutamide
Sulfonylurea

Closes K+ channel in beta-cell membrane so cell depolarizes triggering release of insulin via Ca2+ influx

Stimulates release of endogenous insulin in Type II DM

Requires some islet function so useless in Type I DM

----------------------------------------------
Disulfiram-like effects
Chlorpropamide
Sulfonylurea

Closes K+ channel in beta-cell membrane so cell depolarizes triggering release of insulin via Ca2+ influx

Stimulates release of endogenous insulin in Type II DM

Requires some islet function so useless in Type I DM

----------------------------------------------
Disulfiram-like effects
Glyburide
Sulfonylurea

Closes K+ channel in beta-cell membrane so cell depolarizes trigerring release of insulin via Ca2+ influx

Stimulates release of endogenous insulin in Type II DM

Requires some islet function so useless in Type I DM

----------------------------------------------
Hypoglycemia
Glimepiride
Sulfonylurea

Closes K+ channel in beta-cell membrane so cell depolarizes trigerring release of insulin via Ca2+ influx

Stimulates release of endogenous insulin in Type II DM

Requires some islet function so useless in Type I DM

----------------------------------------------
Hypoglycemia
Glipizide
Sulfonylurea

Closes K+ channel in beta-cell membrane so cell depolarizes trigerring release of insulin via Ca2+ influx

Stimulates release of endogenous insulin in Type II DM

Requires some islet function so useless in Type I DM

----------------------------------------------
Hypoglycemia
Metformin
Biguanide

Possibly decreases gluconeogenesis, increases glycolysis, decreases serum glucose levels

Overall acts as glucose sensitizer

Oral hypoglycemic

Can be used in patients without islet function

-----------------------------------------
Lactic acidosis
Pioglitazone
Glitazone

Inreases target cell response to insulin

Used as monotherapy in Type II DM or combined

-------------------------------------------------
Weight gain

Hepatotoxicity

Cardiovascular toxicity
Rosiglitazone
Glitazone

Inreases target cell response to insulin

Used as monotherapy in Type II DM or combined

-------------------------------------------------
Weight gain

Hepatotoxicity

Cardiovascular toxicity
Acarbose
alpha-glucosidase Inhibitor

Inhibits intestinal brush border alpha-glucosidases

Delayed sugar hydrolysis and glucose absorption leads to decreased postprandial hyperglycemia

Used as monotherapy in Type II DM or in combination

-------------------------------------------
GI disturbances
Miglitol
alpha-glucosidase Inhibitor

Inhibits intestinal brush border alpha-glucosidases

Delayed sugar hydrolysis and glucose absorption leads to decreased postprandial hyperglycemia

Used as monotherapy in Type II DM or in combination

-------------------------------------------
GI disturbances
Pramlintide
Mimetic

Decreases Glucagon

Type II DM

-------------------------------------------
Hypoglycemia

Nausea

Diarrhea
Exenatide
GLP-1 Mimetic

Increases Insulin

Decreases Glucagon release

Type II DM

--------------------------------------------
Pancreatitis?

Nausea

Vomiting
Orlistat
Alters fat metabolism by inhibiting pancreatic lipases

Long-term obesity management (with modified diet)

Orlistat gets rid of FAT

-------------------------------------------
Steatorrhea

GI discomfort

Reduced ADEK absorption

Headache
Sibutramine
Sympathomimetic Serotonin and NE reuptake inhibitor

Short-term and long-term obesity management

-------------------------------------------
Hypertension

Tachycardia
Propylthiouracil
Inhibit organification and coupling of thyroid hormone synthesis

Decreases peripheral conversion of T4 to T3

Hyperthyroidism

-------------------------------------------
Skin rash

Agranulocytosis

Aplastic anemia
Methimazole
Inhibit organification and coupling of thyroid hormone synthesis

Hyperthyroidism

-------------------------------------------
Skin rash

Agranulocytosis

Aplastic anemia
GH
GH Deficiency

Turner's Syndrome
Somatostatin (Octreotide)
Acromegaly

Carcinoid

Gastrinoma

Glucagonoma
Oxytocin
Stimulates labor, uterine contractions, milk let-down

Controls uterine hemorrhage
ADH (desmopressin)
Pituitary CENTRAL diabetes insipidus
Levothyroxine
Thyroxine replacement

Hypothyroidism

Myxedema

-----------------------------------------------
Tachycardia

Heat intolerance

Tremors

Arrhythmias
Triiodothyronine
Thyroxine replacement

Hypothyroidism

Myxedema

-----------------------------------------------
Tachycardia

Heat intolerance

Tremors

Arrhythmias
Hydrocortisone
Decreases production of leukotrienes and prostaglandins by inhibiting Phospholipase A2 and expression of COX-2

Addison's Disease

Inflammation

Immune Suppression

Asthma

-------------------------------------------
Cushings Syndrome

Peptic ulcers

Diabetes if chronic
Prednisone
Decreases production of leukotrienes and prostaglandins by inhibiting Phospholipase A2 and expression of COX-2

Addison's Disease

Inflammation

Immune Suppression

Asthma

-------------------------------------------
Cushings Syndrome

Peptic ulcers

Diabetes if chronic
Triamcinolone
Decreases production of leukotrienes and prostaglandins by inhibiting Phospholipase A2 and expression of COX-2

Addison's Disease

Inflammation

Immune Suppression

Asthma

-------------------------------------------
Cushings Syndrome

Peptic ulcers

Diabetes if chronic
Dexamethasone
Decreases production of leukotrienes and prostaglandins by inhibiting Phospholipase A2 and expression of COX-2

Addison's Disease

Inflammation

Immune Suppression

Asthma

-------------------------------------------
Cushings Syndrome

Peptic ulcers

Diabetes if chronic
Beclomethasone
Decreases production of leukotrienes and prostaglandins by inhibiting Phospholipase A2 and expression of COX-2

Addison's Disease

Inflammation

Immune Suppression

Asthma

-------------------------------------------
Cushings Syndrome

Peptic ulcers

Diabetes if chronic
Demeclocycline
ADH antagonist

Member of tetracycline family

SIADH

----------------------------------------------
Photosensitivity

Abnormal bone and teeth

Nephrogenic Diabetes Insipidus
Cimetidine
H2 Blocker

Reversible block of histamine H2 receptors decreases H+ secretion by parietal cells

Peptic ulcer

Gastritis

Esophageal Reflux

--------------------------------------------
Inhibits CYP450

Prolactin release

Gynecomastia

Impotence

Decreased libido

Can cross BBB (confusion, dizziness, headache)

Can cross placenta

Decrease renal excretion of creatinine
Ranitidine
H2 Blocker

Reversible block of histamine H2 receptors decreases H+ secretion by parietal cells

Peptic ulcer

Gastritis

Esophageal Reflux

-----------------------------------------------
Decrease renal excretion of creatinine
Famotidine
H2 Blocker

Reversible block of histamine H2 receptors decreases H+ secretion by parietal cells

Peptic ulcer

Gastritis

Esophageal Reflux
Nizatidine
H2 Blocker

Reversible block of histamine H2 receptors decreases H+ secretion by parietal cells

Peptic ulcer

Gastritis

Esophageal Reflux
Omeprazole
Proton Pump Inhibitor

Irreversibly inhibits H/K ATPase in stomach parietal cells

Peptic ulcers

Gastritis

Esophageal reflux

Zollinger-Ellison Syndrome
Lansoprazole
Proton Pump Inhibitor

Irreversibly inhibits H/K ATPase in stomach parietal cells

Peptic ulcers

Gastritis

Esophageal reflux

Zollinger-Ellison Syndrome
Bismuth
Binds to ulcer base providing physical protection and allows HCO3- secretion to reestablish pH gradient in mucous layer

Increase ulcer healing

Traveler's diarrhea
Sucralfate
Binds to ulcer base providing physical protection and allows HCO3- secretion to reestablish pH gradient in mucous layer

Increase ulcer healing

Traveler's diarrhea
Misoprostol
A PGE1 analog that increases production and secretion of gastric mucous barrier

Decreases acid production

Prevention of NSAID-induced peptic ulcers

Maintenane of patent ductus arteriosus

Induces labor

--------------------------------------------
Diarrhea

Contraindicated in women of child-bearing age (abortifacient)
Pirenzepine
Blocks M1 receptors on ECL cells to decrease Histamine secretion and M3 receptors on parietal cells to decrease H+ secretion

Peptic ulcers

--------------------------------------------
Tachycardia

Dry mouth

Difficulty focusing eyes
Propantheline
Blocks M1 receptors on ECL cells to decrease Histamine secretion and M3 receptors on parietal cells to decrease H+ secretion

Peptic ulcers

--------------------------------------------
Tachycardia

Dry mouth

Difficulty focusing eyes
Aluminum Hydroxide
Antacids

-------------------------------------------
Constipation

Hypophosphatemia

Proximal muscle weakness

Osteodystrophy

Seizures

Hypokalemia
Magnesium Hydroxide
Antacids

--------------------------------------------
Diarrhea

Hyporeflexia

Hypotension

Cardiac arrest

Hypokalemia
Calcium Carbonate
Antacids

---------------------------------------------
Hypercalcemia

Rebound acid secretion

Hypokalemia
Infliximab
Monoclonal antibody of TNF, proinflammatory cytokine

Crohn's Disease

Rheumatoid arthritis

--------------------------------------------
Respiratory infection (reactivation of latent TB)

Fever

Hypotension
Sulfasalazine
Combination of sulfapyridine (antibacterial) and mesalamine (anti-inflammatory)

Activated by colonic bacteria

Ulcerative colitis

Crohn's Disease

------------------------------------------
Malaise

Nausea

Sulfonamide toxicity

Reversible oligospermia
Odansetron
5-HT3 antagonist

Powerful central-acting antiemetic

Control vomiting post-op and in patients undergoing chemotherapy

--------------------------------------------
Headache

Constipation
Metoclopramide
D2 receptor antagonist

Increases resting tone, contractility, LES tone, motility

Does NOT influence colon transport time

Diabetic and post-surgery gastroparesis

----------------------------------------------
Parkinson Effects

Restlessness

Drowsiness

Fatigue

Depression

Nausea

Diarrhea

Drug interaction with Digoxin and Diabetic agents

Contraindicated in patients with small bowel obstruction
Heparin
Catalyzes the activation of Antithrombin III and decreases thrombin and Xa

Immediate anticoagulation for pulmonary embolism, stroke, MI

Used during pregnancy

Newer LMWH act more on Xa, more bioavailability, longer half-life

-----------------------------------------------
Bleeding

Osteoporosis

Heparin Induce Thrombocytopenia (HIT) = heparin binds to platelets causing antibody production that destroys platelets and overactivates remaining ones, thrombocytopenic hypercoagulable state

Protamine sulfate to reverse
Lepirudin
Hirudin derivative

Directly inhibits thrombin

Alternative to Heparin for anticoagulating patients with HIT
Bivalirudin
Hirudin derivative

Directly inhibits thrombin

Alternative to Heparin for anticoagulating patients with HIT
Warfarin
Interferes with normal synthesis and gamma-carboxylation of Vit. K-dependent clotting factors

Metabolized by CYP450

Increases PT (Extrinsic pathway)

Chronic anticoagulation

Not used in pregnancy

-------------------------------------------
Bleeding

Teratogen

Skin/Tissue Necrosis

Drug-Drug Interactions
Streptokinase
Converts plasminogen to plasmin which cleaves thrombin and fibrin clots

Increases PT and PTT

Early MI, Ischemic stroke

---------------------------------------------
Bleeding

Aminocaproic acid is antidote (inhibits fibrinolysis)
Urokinase
Converts plasminogen to plasmin which cleaves thrombin and fibrin clots

Increases PT and PTT

Early MI, Ischemic stroke

---------------------------------------------
Bleeding

Aminocaproic acid is antidote (inhibits fibrinolysis)
t-PA (Alteplase)
Converts plasminogen to plasmin which cleaves thrombin and fibrin clots

Increases PT and PTT

Early MI, Ischemic stroke

---------------------------------------------
Bleeding

Aminocaproic acid is antidote (inhibits fibrinolysis)
APSAC (Anistreplase)
Converts plasminogen to plasmin which cleaves thrombin and fibrin clots

Increases PT and PTT

Early MI, Ischemic stroke

---------------------------------------------
Bleeding

Aminocaproic acid is antidote (inhibits fibrinolysis)
Aspirin
Acetylates and irreversibly inhibits COX-1 and COX-2 to prevent conversion of arachidonic acid to TXA2

No effect on PT or PTT

Increases Bleeding Time

Antipyretic, Analgesic, Anti-inflammatory, anti-platelet

------------------------------------------------
Gastric ulcers

Bleeding

Hyperventilation

Reye's Syndrome

Tinnitus (CN VIII)
Clopidogrel
Inhibits platelet aggregation by irreversibly blocking ADP receptors

Inhibits fibrinogen by preventing glycoprotein IIb/IIIa expresion

Acute Coronary Syndrome, Coronary Stenting

Decrease incidence/recurrence of thrombotic stroke

----------------------------------------------
Neutropenia
Ticlopidine
Inhibits platelet aggregation by irreversibly blocking ADP receptors

Inhibits fibrinogen by preventing glycoprotein IIb/IIIa expresion

Acute Coronary Syndrome, Coronary Stenting

Decrease incidence/recurrence of thrombotic stroke

----------------------------------------------
Neutropenia
Abciximab
Monoclonal antibody that binds to the glycoprotein receptor IIb/IIIa on activated platelets, preventing aggregation

Acuta Coronary Syndrome, Percutaneous transluminal coronary angioplasty

-------------------------------------------
Bleeding

Thrombocytopenia
Methotrexate
S-phase specific antimetabolite

Folic acid analog that inhibits Dihydrofolate reductase causing decreased dTMP and thus decreased DNA and protein synthesis

Leukemias / Lymphomas

Choriocarcinoma

Sarcoma

Abortion

Ectopic Pregnancy

Rheumatoid Arthritis

Psoriasis

--------------------------------------------
Myelosuppression (reversible with Leucovorin or folinic acid

Macrovesicular fatty change in liver

Mucositis
5-Fluorouracil
S-phase specific antimetabolite

Pyrimidine analog bioactivated to 5F-dUMP which covalently complexes folic acid

Complex inhibits thymidylate synthase causing decreased dTMP and decreased DNA and protein synthesis

Colon cancer and solid tumors

Basal cell carcinoma (topical)

Synergy with Methotrexate

--------------------------------------------
Myelosuppression (NOT reversible with Leucovorin)

Photosensitivity

Rescue with Thymidine
6-Mercaptopurine
Blocks de novo purine synthesis

Activated by HGPRTase

Leukemia / Lymphoma
(NOT CLL or Hodgkin's)

--------------------------------------------
Bone marrow

GI

Liver

Metabolized by Xanthine Oxidase so increased toxicity with Allopurinol
Cytarabine
Inhibits DNA polymerase

AML, ALL

High-grade non-Hodgkin's Lymphoma

-------------------------------------------
Leukopenia

Thrombocytopenia

Megaloblastic anemia
Cyclophosphamide
Alkylating agents

Covalently cross-links (interstrand) DNA at guanine N-7

Requires bioactivation by Liver

Non-Hodgkin's Lymphoma

Breast / Ovarian Carcinomas

Immunosuppressant

------------------------------------------
Myelosuppression

Hemorrhagic Cystitis (prevent with Mesna)
Ifosfamide
Alkylating agents

Covalently cross-links (interstrand) DNA at guanine N-7

Requires bioactivation by Liver

Non-Hodgkin's Lymphoma

Breast / Ovarian Carcinomas

Immunosuppressant

------------------------------------------
Myelosuppression

Hemorrhagic Cystitis (prevent with Mesna)
Carmustine
Nitrosourea

Alkylate DNA

Require bioactivation

Cross BBB to CNS

Brain tumors (including glioblastoma multiforme)

---------------------------------------------
CNS Toxicity (dizziness, ataxia)
Lomustine
Nitrosourea

Alkylate DNA

Require bioactivation

Cross BBB to CNS

Brain tumors (including glioblastoma multiforme)

---------------------------------------------
CNS Toxicity (dizziness, ataxia)
Semustine
Nitrosourea

Alkylate DNA

Require bioactivation

Cross BBB to CNS

Brain tumors (including glioblastoma multiforme)

---------------------------------------------
CNS Toxicity (dizziness, ataxia)
Streptozocin
Nitrosourea

Alkylate DNA

Require bioactivation

Cross BBB to CNS

Brain tumors (including glioblastoma multiforme)

---------------------------------------------
CNS Toxicity (dizziness, ataxia)
Cisplatin
Cross-links DNA

Testicular Carcinoma

Bladder Carcinoma

Ovarian Carcinoma

Lung Carcinoma

--------------------------------------------
Nephrotoxicity

Acoustic nerve damage
Carboplatin
Cross-links DNA

Testicular Carcinoma

Bladder Carcinoma

Ovarian Carcinoma

Lung Carcinoma

--------------------------------------------
Nephrotoxicity

Acoustic nerve damage
Busulfan
Alkylates DNA

CML

Ablating bone marrow in hematopoietic stem cell transplants

-------------------------------------------
Pulmonary fibrosis

Hyperpigmentation
Doxorubicin (Adriamycin)
Generates free radicals and noncovalently intercalates in DNA (creating breaks in DNA strand to decrease replication)

ABVD Regimen for Hodgkin's Lymphoma

Myeloma

Sarcoma

Breast / Ovary / Lung tumors

--------------------------------------------
Cardiotoxicity

Myelosuppression

Marked alopecia

Toxic extravasation
Daunorubicin
Generates free radicals and noncovalently intercalates in DNA (creating breaks in DNA strand to decrease replication)

ABVD Regimen for Hodgkin's Lymphoma

Myeloma

Sarcoma

Breast / Ovary / Lung tumors

--------------------------------------------
Cardiotoxicity

Myelosuppression

Marked alopecia

Toxic extravasation
Dactinomycin (Actinomycin D)
Intercalates in DNA

Wilm's Tumor

Ewing's Sarcoma

Rhabdomyosarcoma

ACTinomycin since kids ACT out

-------------------------------------------
Myelosuppression
Bleomycin
Induces formation of free radicals, which cause breaks in DNA strands

Testicular cancer

Hodgkin's Lymphoma (ABVD Regimen)

---------------------------------------------
Pulmonary fibrosis

Skin changes

Minimal myelosuppression
Hydroxyurea
Inhibits Ribonucleotide reductase
and so decreases DNA synthesis (S-phase specific)

Melanoma

CML

Sickle Cell Disease (increases HbF)

---------------------------------------------
Bone marrow suppression

GI Upset
Etoposide (VP-16)
G2-phase specific agent that inhibits Topoisomerase II and increases DNA degradation

Small Cell Lung Cancer

Small Cell Prostate Cancer

Testicular Carcinoma

-------------------------------------------
Myelosuppression

GI Irritation

Alopecia
Prednisone
May trigger apoptosis, may even work on non-dividing cells

Cancer chemotherapy

CLL

Hodgkin's Lymphoma (MOPP Regimen)

Immunosupression in autoimmune diseases

------------------------------------------
Cushing-like Symptoms

Immunosuppression

Cataracts

Acne

Osteoporosis

Hypertension

Peptic ulcers

Hyperglycemia

Psychosis
Tamoxifen
SERMs

receptor antagonists in breast
receptor agonist in bone

Block the binding of estrogen to estrogen receptor + cells

Breast cancer

Prevent Osteoporosis

-----------------------------------------------
Increase Endometrial carcinoma via partial agonist effects

Hot flashes
Raloxifene
SERMs

receptor antagonists in breast
receptor agonist in bone

Block the binding of estrogen to estrogen receptor + cells

Breast cancer

Prevent Osteoporosis

-----------------------------------------------
Hot flashes
Trastuzumab (Herceptin)
Monoclonal antibody against HER-2 (erb-B2)

Helps kill breast cancer cells that overexpress HER-2 possibly through antibody-dependent cytotoxicity (ADCC)

Metastatic breast cancer

-----------------------------------------
Cardiotoxicity
Imatinib (Gleevac)
Philadelpia chromosome bcr-abl tyrosine kinase inhibitor

CML

GI stromal tumors

------------------------------------------
Fluid retention
Vincristine
M-phase specific alkaloids that bind to tubulin and block polymerization of microtubules so that mitotic spindle cannot form

Part of MOPP Regimen for Hodgkin's Lymphoma

Wilm's Tumor

Choriocarcinoma

-------------------------------------------
Neurotoxicity (areflexia, peripheral neuritis)

Paralytic ileus
Vinblastine
M-phase specific alkaloids that bind to tubulin and block polymerization of microtubules so that mitotic spindle cannot form

Part of MOPP Regimen for Hodgkin's Lymphoma

Wilm's Tumor

Choriocarcinoma

-------------------------------------------
Bone marrow suppression
Paclitaxel
Taxol

M-phase specific agent that binds to tubulin and hyperstabilize polymerized microtubules so the mitotic spindle cannot break down (anaphase cannot occur)

Ovarian / Breast carcinomas

--------------------------------------------
Myelosuppression

Hypersensitivity
Aspirin
Irreversibly inhibits COX by covalent binding which decreases synthesis of both Thromboxane and Prostaglandins

Low dose to decrease platelet aggregation (<300mg-2400gm)

----------------------------------------------
Gastric upset

Acute renal failure

Interstitial nephritis

Upper GI bleeding

Reye's Syndrome in children with viral infection
Ibuprofen
NSAID

Reversibly inhibits COX-1 and COX-2

Blocks Prostaglandin synthesis

Antipyretic

Analgesic

Anti-inflammatory

------------------------------------------
Renal damage

Aplastic anemia

GI distress

Ulcers
Naproxen
NSAID

Reversibly inhibits COX-1 and COX-2

Blocks Prostaglandin synthesis

Antipyretic

Analgesic

Anti-inflammatory

------------------------------------------
Renal damage

Aplastic anemia

GI distress

Ulcers
Indomethacin
NSAID

Reversibly inhibits COX-1 and COX-2

Blocks Prostaglandin synthesis

Close patent ductus arteriosus

Antipyretic

Analgesic

Anti-inflammatory

------------------------------------------
Renal damage

Aplastic anemia

GI distress

Ulcers
Ketorolac
NSAID

Reversibly inhibits COX-1 and COX-2

Blocks Prostaglandin synthesis

Antipyretic

Analgesic

Anti-inflammatory

------------------------------------------
Renal damage

Aplastic anemia

GI distress

Ulcers
Celecoxib
COX-2 Inhibitor

Reversibly inhibits COX-2 found in inflammatory cells and vascular endothelium and mediates inflammation and pain

Spares COX-1 so maintains gastric mucosa

Rheumatoid arthritis

Osteoarthritis

------------------------------------------
Increased thrombosis

Sulfa allergy

Less ulcers and bleeding than NSAIDs
Acetaminophen
Reversibly inhibits COX, mostly in CNS

Inactivated peripherally

Antipyretic, Analgesic

NO anti-inflammatory

Used in children to prevent Reye's Syndrome in viral infection

-------------------------------------------
Hepatic necrosis in overdose

Metabolite depletes Glutathione and forms toxic tissue adducts in liver

N-acetylcysteine is antidote (regenerates glutathione)
Etridronate
Bisphosphonate

Inhibits osteoclastic activity

Reduces formation and resorption of hydroxyapatite

Malignancy-associated hypercalcemia

Paget's Disease of bone

Postmenopausal osteoporosis

-------------------------------------------
Corrosive esophagitis

Nausea

Diarrhea
Pamidronate
Bisphosphonate

Inhibits osteoclastic activity

Reduces formation and resorption of hydroxyapatite

Malignancy-associated hypercalcemia

Paget's Disease of bone

Postmenopausal osteoporosis

-------------------------------------------
Corrosive esophagitis

Nausea

Diarrhea
Alendronate
Bisphosphonate

Inhibits osteoclastic activity

Reduces formation and resorption of hydroxyapatite

Malignancy-associated hypercalcemia

Paget's Disease of bone

Postmenopausal osteoporosis

-------------------------------------------
Corrosive esophagitis

Nausea

Diarrhea
Risedronate
Bisphosphonate

Inhibits osteoclastic activity

Reduces formation and resorption of hydroxyapatite

Malignancy-associated hypercalcemia

Paget's Disease of bone

Postmenopausal osteoporosis

-------------------------------------------
Corrosive esophagitis

Nausea

Diarrhea
Colchicine
Chronic gout

Depolymerizes microtubules impairing leukocyte chemotaxis and degranulation

-------------------------------------------
GI side effects (especially if orally given)

Indomethacin is less toxic for use in acute gout

Salicylates depress uric acid clearance
Probenecid
Chronic gout

Inhibits reabsorption or uric acid in PCT (also inhibits secretion of Penicillin)

Salicylates depress uric acid clearance
Allopurinol
Chronic gout

Inhibits Xanthine oxidase and decreases conversion of xanthine to uric acid

Used in Leukemia and Lymphoma to prevent tumor-lysis syndrome-associated urate nephropathy

Increases concentrations of Azathioprine and 6-MP (both normally metabolized by Xanthine oxidase)

Salicylates depress uric acid clearance
Etanercept
Recombinant form of human TNF receptor that binds TNF

Rheumatoid arthritis

Psoriasis

Ankylosing spondylitis
Infliximab
Anti-TNF antibody

Crohn's Disease

Rheumatoid arthritis

Ankylosing spondylitis
Mannitol
Osmotic diuretic

Increases tubular fluid osmolarity producing increased urine flow

Shock

Drug overdose

Decrease intracranial/intraocular pressure

-----------------------------------------
Pulmonary edema

Dehydration

Contraindicated in anuria, CHF
Acetazolamide
Carbonic anhydrase inhibitor

Causes self-limited NAHCO3 diuresis and reduction in total body HCO3-

Glaucoma

Urinary alkalinization

Metabolic alkalosis

Altitude sickness

-------------------------------------------
Hyperchloremic metabolic acidosis

Neuropathy

NH3 toxicity

Sulfa allergy

ACIDazolamid causes acidosis
Furosemide
Sulfonamide loop diuretic

Inhibits cotransport system (Na/K/2Cl) of thick ascending limb

Abolishes hypertonicity of medulla, prevents concentrating of urine

Increases Ca2+ excretion (Loops lose calcium)

Edematous states (CHF, cirrhosis, nephrotic syndrome, pulmonary edema)

Hypertension

Hypercalcemia

----------------------------------------------
Ototoxicity

Hypokalemia

Dehydration

Sulfa allergy

Interstitial nephritis

Gout

OH DANG
Ethacrynic Acid
Phenoxyacetic acid derivative (NOT a sulfonamide)

Inhibits cotransport system (Na/K/2Cl) of thick ascending limb

Abolishes hypertonicity of medulla, prevents concentrating of urine

Increases Ca2+ excretion (Loops lose calcium)

Diuresis in patient allergic to sulfa drugs

-------------------------------------------------
Ototoxicity

Hypokalemia

Dehydration

Interstitial nephritis

Gout

Can be used in hyperuricemia

OH DANG
Hydrochlorothiazide
Thiazide diuretic

Inhibits NaCl reabsorption in early distal tubule, reducing diluting capacity of the nephron

Decreases Ca2+ excretion

Hypertension

CHF

Idiopathic hypercalciuria

Nephrogenic diabetes insipidus

----------------------------------------------
Hypokalemic metabolic acidosis

Hyponatremia

Hyperglycemia

Hyperlipidemia

Hyperuricemia

Hypercalcemia

HyperGLUC

Sulfa allergy
Spironolactone
Competitive adlosterone receptor antagonist on the cortical collecting tubule

Hyperaldosteronism

K+ depletion

CHF

-------------------------------------------------
Hyperkalemia (can lead to arrhythmias)

Endocrine effects (gynecomastia, antiandrogen effects)
Triamterene
Blocks Na+ channels in cortical collecting tubule

Hyperaldsteronism

K+ depletion

CHF

-------------------------------------------------
Hyperkalemia (can lead to arrhythmias)

Endocrine effects (gynecomastia, antiandrogen effects)
Amiloride
Blocks Na+ channels in cortical collecting tubule

Hyperaldsteronism

K+ depletion

CHF

-------------------------------------------------
Hyperkalemia (can lead to arrhythmias)

Endocrine effects (gynecomastia, antiandrogen effects)
Eplerenone
Blocks Na+ channels in cortical collecting tubule

Hyperaldsteronism

K+ depletion

CHF

-------------------------------------------------
Hyperkalemia (can lead to arrhythmias)

Endocrine effects (gynecomastia, antiandrogen effects)
Captopril
ACE Inhibitor

Inhibits ACE reducing levels of angiotensin II and preventing inactivation of bradykinin (a vasodilator)

Increases renin due to loss of feeedback

Hypertension

CHF

Diabetic renal disease

-------------------------------------------------
Cough

Angioedema

Proteinuria

Taste changes

Hypotension

Teratogen (fetal renal damage)

Increased renin

Hyperkalemia

Avoid with bilateral renal artery stenosis because ACE inhibitors reduce GFR by preventing constriction of efferent arterioles

CAPTOPRIL
Enalapril
ACE Inhibitor

Inhibits ACE reducing levels of angiotensin II and preventing inactivation of bradykinin (a vasodilator)

Increases renin due to loss of feeedback

Hypertension

CHF

Diabetic renal disease

-------------------------------------------------
Cough

Angioedema

Proteinuria

Taste changes

Hypotension

Teratogen (fetal renal damage)

Increased renin

Hyperkalemia

Avoid with bilateral renal artery stenosis because ACE inhibitors reduce GFR by preventing constriction of efferent arterioles

CAPTOPRIL
Lisinopril
ACE Inhibitor

Inhibits ACE reducing levels of angiotensin II and preventing inactivation of bradykinin (a vasodilator)

Increases renin due to loss of feeedback

Hypertension

CHF

Diabetic renal disease

-------------------------------------------------
Cough

Angioedema

Proteinuria

Taste changes

Hypotension

Teratogen (fetal renal damage)

Increased renin

Hyperkalemia

Avoid with bilateral renal artery stenosis because ACE inhibitors reduce GFR by preventing constriction of efferent arterioles

CAPTOPRIL
Finasteride (Propecia)
5-alpha reductase inhibitor

Decreases conversion of testosterone to DHT

BPH

Promotes hair growth (used in male-pattern baldness)

------------------------------------------
To prevent baldness, give a drug that encourages female breast growth
Flutamide
A nonsteroidal competitive inhibitor of androgens at the testosterone receptor

Prostate carcinoma
Ketoconazole
Inhibits steroid synthesis

PCOS to prevent hirsutism

-------------------------------------------
Gynecomastia

Amenorrhea
Spironolactone
Inhibits steroid binding

PCOS to prevent hirsutism

-------------------------------------------
Gynecomastia

Amenorrhea
Leuprolide
GnRH analog with agonist properties when used in pusatile fashion; antagonist properties when used in continuous fashion

Infertility (pulsatile)

Prostate cancer (continuous)

Uterine fibroids

-------------------------------------------
Antiandrogen

Nausea

Vomiting

Leuprolide used in LIEU or GnRH
Sildenafil
Inhibits cGMP phosphodiesterase causing increased smooth muscle relaxation in the corpus cavernosum

Increases blood flow

Erectile dysfunction

---------------------------------------------
Headache

Flushing

Dyspepsia

Impaired blue-green vision

Life-threatening hypotension with Nitrates
Vardenafil
Inhibits cGMP phosphodiesterase causing increased smooth muscle relaxation in the corpus cavernosum

Increases blood flow

Erectile dysfunction

---------------------------------------------
Headache

Flushing

Dyspepsia

Impaired blue-green vision

Life-threatening hypotension with Nitrates
Mifepristone (RU-486)
Competitive inhibitor of progestins at progesterone receptors

Termination of pregnancy (given with Misoprostol [PGE1])

------------------------------------------------
Heavy bleeding

GI effects (nausea, vomiting, anorexia)

Abdominal pain
Oral Contraceptives (synthetic progestins, estrogen)
Prevent estrogen surge and thus prevent LH surge so ovulation does not occur

Reliable

Decreased risk of ovarian / endometrial cancer

Decreased ectopic pregnancy

Decreased pelvic infections

Regulates menses

-------------------------------------------
Taken daily

No protection against STDs

Increases TG

Depression

Weight gain

Hypertension

Nausea

Hypercoagulable state
Hormone Replacement Therapy
Used for relief or prevention of menopausal symptoms (hot flashes, vaginal atrophy) and osteoporosis (due to decreased E2)

-----------------------------------------------
Unopposed estrogen therapy increases risk of endometrial carcinoma so progesterone is added

Increased cardiovascular risk
Dinoprostone
PGE2 analog causing cervical dilation and uterine contraction

Induces labor
Ritrodine
Beta-2 agonist that relaxes the uterus

Reduces premature uterine contractions
Terbutaline
Beta-2 agonist that relaxes the uterus

Reduces premature uterine contractions
Testosterone (Methyltestosterone)
Agonist at androgen receptors

Treats hypogonadism and promotes development of 2º sex chraracteristics

Stimulates anabolism to promote recovery after burn or injury

Treats estrogen-receptor + breast cancer (exemestane)

---------------------------------------------
Masculinization in females

Reduces intratesticular testosterone in males by inhibiting Leydig cells (leads to gonadal atrophy)

Premature closure of epiphyseal plates
Anastrazole
Aromatase inhibitor used in postmenopausal women with breast cancer
Exemestane
Aromatase inhibitor used in postmenopausal women with breast cancer
Ethinyl estradiol
Binds estrogen receptors

Hypogonadism in ovarian failure

Menstrual abnormalities

HRT in postmenopausal women

Used in men with androgen-dependent prostate cancer

------------------------------------------
Increases risk of endometrial cancer

Increases bleeding in postmenopausal women

Increases thrombi risk

Contraindicated in estrogen receptor + breast cancer
DES
Binds estrogen receptors

Hypogonadism in ovarian failure

Menstrual abnormalities

HRT in postmenopausal women

Used in men with androgen-dependent prostate cancer

------------------------------------------
Increases risk of endometrial cancer

Increases bleeding in postmenopausal women

Increases thrombi risk

Contraindicaed in estrogen receptor + breast cancer

Clear cell adenocarcinoma of vagina in females exposed to DES in utero
Mestranol
Binds estrogen receptors

Hypogonadism in ovarian failure

Menstrual abnormalities

HRT in postmenopausal women

Used in men with androgen-dependent prostate cancer

------------------------------------------
Increases risk of endometrial cancer

Increases bleeding in postmenpausal women

Increases thrombi risk

Contraindicaed in estrogen receptor + breast cancer
Progestin
Binds progesterone receptors

Reduces growth

Increases vascularization of endometrium

Used in oral contraceptives

Treats endometrial cancer

Treats abnormal uterine bleeding
Clomiphene
SERM

Partial agonist at estrogen receptors in pituitary gland

Prevents feedback inhibition and increases release of LH and FSH from pituitary which stimulates ovulation

Treats infertility and PCOS

--------------------------------------------
Hot flashes

Ovarian enlargement

Multiple spontaneous pregnancies

Visual disturbances
Tamoxifen
Antagonist on breast tissue

Treats and Prevents recurrence of estrogen receptor + breast cancer
Raloxifene
Agonist on bone

Reduces resorption of bone

Used to treat osteoporosis
Diphenhydramine
1st Generation H1 blocker

Allergy

Motion sickness

Sleep aid

--------------------------------------------
Sedation

Anti-muscarinic

Anti-alpha adrenergic
Dimenhydrinate
1st Generation H1 blocker

Allergy

Motion sickness

Sleep aid

--------------------------------------------
Sedation

Anti-muscarinic

Anti-alpha adrenergic
Chlorpheniramine
1st Generation H1 blocker

Allergy

Motion sickness

Sleep aid

--------------------------------------------
Sedation

Anti-muscarinic

Anti-alpha adrenergic
Loratadine
2nd Generation H1 Blocker

Allergy

--------------------------------------------
Less sedation (decreased entry into CNS)
Fexofenadine
2nd Generation H1 Blocker

Allergy

--------------------------------------------
Less sedation (decreased entry into CNS)
Desloratadine
2nd Generation H1 Blocker

Allergy

--------------------------------------------
Less sedation (decreased entry into CNS)
Cetirizine
2nd Generation H1 Blocker

Allergy

--------------------------------------------
Less sedation (decreased entry into CNS)
Isoproterenol
Relaxes bronchial smooth muscle (beta-2)

Asthma

------------------------------------------
Tachycardia (beta-1)
Albuterol
Relaxes bronchial smooth muscle (beta-2)

Use during acute exacerbation

Asthma
Salmeterol
Relaxes bronchial smooth muscle (beta-2)

Long-acting agent for prophylaxis

Asthma

--------------------------------------------
Tremor

Arrhythmia
Theophylline
Methylxanthine

Bronchodilation by inhibiting phosphodiesterase and decreasing cAMP hydrolysis

Asthma

------------------------------------------
Narrow therapeutic index

Cardiotoxicity

Neurotoxicity

Metabolized by CYP450
Ipratropium
Muscarinic Antagonist

Competitive block of muscarinic receptors preventing bronchoconstriction

Asthma, COPD
Cromolyn
Prevents release of mediators from mast cells

Effective only for the prophylaxis of asthma

Not effective during acute attack

Toxicity is rare
Beclomethasone
Inhibits the synthesis of all cytokines

Inactives NF-kB, the transcription factor that induces the production of TNF-alpha and others

1st line treatment for chronic asthma
Prednisone
Inhibits the synthesis of all cytokines

Inactives NF-kB, the transcription factor that induces the production of TNF-alpha and others

1st line treatment for chronic asthma
Zileuton
5-lipoxygenase pathway inhibitor

Blocks conversion or arachidonic acid to leukotrienes
Zafirlukast
Blocks leukotriene receptors

Especially good for aspirin-induced asthma
Montelukast
Blocks leukotriene receptors

Especially good for aspirin-induced asthma
Guafenesin (Robitussin)
Removes excess sputum but large doses necessary

Does not suppress cough reflex
N-acetylcysteine
Mucolytic

Loosens musous plugs in CF patients

Used as antidote for acetaminophen overdose
Hydroxyurea
Inhibits ribonucleotide reductase
6-Mercaptopurine
Blocks de novo purine synthesis
5-Fluorouracil
Inhibits thymidylate synthase
Methotrexate
Inhibits DHF reductase
Trimethoprim
Inhibits DHF reductase
Fluoroquinolones
Inhibit DNA gyrase (prokaryotic topoisomerase)
Tetracyclines
Bind 30S subunit and prevent aminoacyl-tRNA attachment
Aminoglycosides
Inhibit formation of initiation complex and cause misreading of mRNA
Cloramphenicol
Inhibits 50S peptidyltransferase
Macrolides
Bind 50S and blocks translocation
Clindamycin
Binds 50S and blocks translocation
Ouabain
Binds K+ site on Na/K ATPase to inhibit it
Cyclosporine
Binds to cycophilins

Complex blocks the differentiation and activation of T cells by inhibiting calcineurin and thus preventing production of IL-2 and its receptor

Suppresses organ rejection after transplant

Selected autoimmune disorders

---------------------------------------------
Predisposes to viral infections and lymphoma

Nephrotoxic (prevent with mannitol diuresis)
Tacrolimus (FK506)
Binds to FK binding protein and inhibits secretion of IL-2 and other cytokines

Potent immunosuppressive for organ transplants

---------------------------------------------
Nephrtoxicity

Peripheral neuropathy

Hypertension

Pleural effusion

Hyperglycemia
Azathioprine
Antimetabolite precursor of 6-MP that interferes with the metabolism and synthesis of nucleic acids

Toxic to proliferating lymphocytes

Kidney transplants

Autoimmune disorders (glomerulonephritis and hemolytic anemia)

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Bone marrow suppression

6-MP metabolized by Xanthine oxidase so toxic with Allopurinol
Muromonab-CD3 (OKT3)
Monoclonal antibody that binds CD3 (epsilon chain) on the surface of T cells

Blocks cellular interaction with CD3 protein responsible for T-cell signal transduction

Immunosuppression after kidney transplant

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Cytokine release syndrome

Hypersensitivity reaction
Sirolimus (Rapamycin)
Binds to mTOR

Inhibits T cell proliferation in response to IL-2

Immunosuppression after kidney transplant in combo with Cyclosporine and Corticosteroids

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Hyperlipidemia

Thrombocytopenia

Leukopenia
Mycophenolate Mofetil
Inhibits de novo guanine synthesis and blocks lymphocyte production
Daclizumab
Monoclonal antibody with high affinity for IL-2 receptor on activated T cells
Aldesleukin (IL-2)
Recombinant IL-2

Renal cell carcinoma

Metastatic Melanoma
Erythropoietin (Epoietin)
Anemias (especially in renal failure)
Filgastrim (G-CSF)
Recovery of bone marrow
Sargramostim (GM-CSF)
Recovery of bone marrow
alpha-Interferon
Hepatitis B / C

Kaposi's Sarcoma

Leukemias

Malignant Melanoma
beta-Interferon
Multiple Sclerosis
gamma-Interferon
Chronic granulomatous disease
Oprelvekin (IL-11)
Thrombocytopenia
Thrombopoietin
Thrombocytopenia