Drug overview

Last updated: August 13, 2024

Summary

This article gives an overview of the most important classes of drugs used for each system (e.g., the cardiovascular system), as well as the most common drugs that are used in the treatment of specific conditions (e.g., Parkinson disease).

Analgesics

Overview
Agents		Indications	Mechanism of action	Adverse effects		Contraindications	Interactions
Nonopioid analgesics
Nonsteroidal anti-inflammatory drugs (NSAIDs)	Ibuprofen, diclofenac, indomethacin, naproxen ^[1]	Acute and chronic pain	Reversible inhibition of the enzymes COX-1 and COX-2 → ↓ prostaglandin synthesis → analgesic, antipyretic, anti-inflammatory, and minor antiplatelet effects	Gastrointestinal (most common), e.g., dyspepsia, gastric ulceration, hemorrhage) Analgesic nephropathy Aplastic anemia	↑ Risk of heart attack and stroke	Gastroduodenal ulcers Renal failure Pregnancy Acute hemorrhage (especially aspirin)	Anticoagulants, antiplatelets: ↑ risk of bleeding MTX: ↑ bone marrow toxicity	Increase plasma levels of lithium ACEIs: ↓ antihypertensive effect; kidney failure
Nonsteroidal anti-inflammatory drugs (NSAIDs)	Aspirin ^[2]	Acute myocardial infarction, stroke Angina Primary prevention and management of ASCVD	Irreversible COX-1 and COX-2 inhibition → antipyretic, anti-inflammatory, and analgesic effects Irreversible COX-1 inhibition → inhibition of TXA2 synthesis in platelets → inhibition of platelet aggregation (antithrombotic effect)		Salicylate toxicity Tinnitus			Decreases phenytoin concentration
COX-2 inhibitors (selective NSAIDs, e.g., celecoxib) ^[3]		Rheumatoid arthritis, osteoarthritis	Reversible selective inhibition of COX-2 with almost no inhibition of COX-1 → analgesic and anti-inflammatory effects	↑ Risk of thrombosis, MI, and/or stroke Sulfa drug allergy		Severe heart failure, recent myocardial infarction Gastrointestinal bleeding	ACEIs, ARBs: ↓ antihypertensive effect; kidney failure Anticoagulants, antiplatelets, SSRIs, SNRIs: ↑ risk of bleeding Increase digoxin serum concentration
Acetaminophen		Fever and pain during pregnancy and in pediatric patients	Reversibly inhibits cyclooxygenase, mainly in the CNS → analgesic and antipyretic effects	Minimal gastric side effects Hepatotoxicity due to acetaminophen overdose		Severe liver impairment	CYP2E1 inhibitors: ↑ acetaminophen concentration → ↑ hepatotoxicity
Metamizole		Not available in the US (withdrawn)	Not completely understood Thought to inhibit central cyclooxygenases and activate endogenous pain-modulating systems → analgesic, antipyretic, and spasmolytic effects	Agranulocytosis Allergic reactions		History of hypersensitivity to the drug or aspirin-exacerbated respiratory disease Pregnancy	MTX: ↑ risk of hematologic toxicity
Opioid analgesics
Low-potency opioids (e.g., codeine, tramadol)		Acute and chronic pain management Management of cough and diarrhea Treatment of opioid use disorder	Agonism at heptahelical GPCRs μ, δ, and/or κ → ↓ synaptic transmission Presynaptic inhibition → ↓ release of transmitters (e.g., substance P, noradrenaline, serotonin) Postsynaptic inhibition → hyperpolarization μ-opioid receptor: strong analgesia, slowed gastrointestinal transit δ-opioid receptor: analgesia κ-opioid receptor: analgesia, sedation	Respiratory depression CNS depression Euphoria Strong addictive potential		Intoxication (e.g., alcohol, sedatives) Lung disease (e.g., asthma, chronic bronchitis) Gastrointestinal conditions (e.g., paralytic ileus, IBD) Psychiatric conditions (e.g., suicidality) Hypersensitivity	Interactions vary according to the opioid but can include: Serotonergic drugs: ↑ risk of serotonin syndrome (tramadol, meperidine) Other opiods: receptor displacement (buprenorphine)
Medium-potency opioids (e.g., morphine, oxycodone, methadone)
High-potency opioids (e.g., fentanyl, buprenorphine)

Antimicrobial drugs

This section provides an overview of the most important antimicrobial drug classes and substances.

Antibiotics

Overview
Agents			Indications	Mechanism of action	Adverse effects
Inhibition of cell wall synthesis
β-lactams	Penicillins	Natural penicillins (e.g., penicillin G and penicillin V)	Gram-positive aerobes, branching gram-positive anaerobes Gram-negative cocci Spirochetes	See “Overview of antibiotics” for details.	Hypersensitivity Interstitial nephritis	Hemolytic anemia
		Antistaphylococcal penicillins (e.g., oxacillin)	Gram-positive aerobes (especially Staphylococcus aureus)			Pseudomembranous colitis	Large doses: neurotoxicity ^[4] Hepatotoxicity
		Aminopenicillins (e.g., amoxicillin, ampicillin)	Helicobacter pylori, Escherichia coli, Salmonella, Shigella, Enterococci Haemophilus influenzae, Listeria monocytogenes			Pseudomembranous colitis	Diarrhea
		Antipseudomonal penicillins (e.g., piperacillin, ticarcillin)	Gram-negative rods, especially Pseudomonas			Headache, insomnia ^[5]	Diarrhea
	Cephalosporins	First-generation (e.g., cephalexin)	See “Overview of clinical use of cephalosporins” for details.		Potential cross-reactivity in patients with penicillin allergies, disulfiram-like reaction AIHA Vitamin K deficiency
		Second-generation (e.g., cefaclor)
		Third-generation (e.g., cefixime)
		Fourth-generation (e.g., cefepime)
		Fifth-generation (ceftaroline)
	Carbapenems (e.g., imipenem, meropenem)		Last-resort drugs Gram-positive cocci (except for MRSA) Gram-negative rods, including Pseudomonas aeruginosa Anaerobes		CNS toxicity: ↓ seizure threshold (imipenem > meropenem) Gastrointestinal upset, rash
	Monobactams (e.g., aztreonam)		Gram-negative bacteria only Alternative for penicillin-allergic patients		Gastrointestinal upset
Glycopeptides (e.g., vancomycin)			Wide range of multidrug-resistant gram-positive bacteria (e.g., MRSA, Clostridioides difficile)		Nephrotoxicity, ototoxicity Vancomycin flushing reaction, thrombophlebitis DRESS syndrome
Epoxides (e.g., fosfomycin)			Women with uncomplicated UTIs		Mild electrolyte imbalances Diarrhea
Disruption of cell membrane integrity
Lipopeptides (e.g., daptomycin)			Gram-positive bacteria, especially MRSA, VRE Main uses: skin infections, bacteremia, and endocarditis	See “Overview of antibiotics” for details.	Reversible myopathy, rhabdomyolysis
Polymyxins (e.g., colistin, polymyxin B)			Severe infections caused by multidrug-resistant gram-negative bacteria (e.g., P. aeruginosa, Acinetobacter baumannii)	See “Overview of antibiotics” for details.	Nephrotoxicity, neurotoxicity Respiratory failure
Inhibition of protein synthesis: 30S ribosomal subunit
Aminoglycosides (e.g., gentamicin, streptomycin, neomycin)			Severe gram-negative rod infections (not effective against anaerobes)	See “Overview of antibiotics” for details.	Nephrotoxicity; ototoxicity and vestibulotoxicity Neuromuscular blockade Teratogenicity
Tetracyclines (e.g., tetracycline, doxycycline)			Intracellular bacteria, such as Rickettsia, Chlamydia Community-acquired MRSA (doxycycline)		Deposition in bones and teeth Photosensitivity Gastrointestinal upset	Associated with Fanconi syndrome
Glycylcylines (tetracyclin derivative; e.g., tigecycline)			Gram-positive aerobes (MRSA, VRE), gram-negative aerobes Anaerobes			Hepatotoxicity
Inhibition of protein synthesis: 50S ribosomal subunit
Macrolides and ketolides (e.g., erythromycin, clarithromycin, azithromycin)			Atypical pneumonia Bordetella pertussis STIs caused by Chlamydia	See “Overview of antibiotics” for details.	QT-interval prolongation, arrhythmia ↑ Risk of hypertrophic pyloric stenosis in infants ≤ 6 weeks of age
Lincosamides (e.g., clindamycin)			Anaerobes, such as Clostridium perfringens, Bacteroides spp. Group A streptococcus: especially invasive infections		Gastrointestinal upset Pseudomembranous colitis
Streptogramins (quinupristin-dalfopristin)			Skin and skin structure infection with S. aureus (MSSA, MRSA), Streptococcus pyogenes, vancomycin-resistant Enterococcus faecium		Arthralgia, myalgia Thrombophlebitis Rash, pruritus
Oxazolidinones (linezolid)			Multidrug-resistant gram-positive bacteria (VRE, MRSA)		Bone marrow suppression → pancytopenia Peripheral neuropathy Serotonin syndrome
Amphenicols (chloramphenicol)			Meningitis caused by H. influenzae, Neisseria meningitidis, and/or Streptococcus pneumoniae Rickettsia infections		Dose-dependent bone marrow suppression → aplastic anemia Gray baby syndrome
DNA gyrase inhibition
Fluoroquinolones (e.g., ciprofloxacin, levofloxacin)			Ciprofloxacin: P. aeruginosa Levofloxacin: atypical bacteria (e.g., Legionella spp., Mycoplasma spp.)	See “Overview of antibiotics” for details.	Hyperglycemia/hypoglycemia QT prolongation Adults: tendon rupture, especially of the Achilles tendon Children: potential damage to growing cartilage → reversible arthropathy
Disruption of DNA integrity
Nitroimidazoles (e.g., metronidazole)			Certain protozoa (e.g., Entamoeba histolytica, Giardia, Trichomonas) Facultative anaerobes (Gardnerella vaginalis, H. pylori)	See “Overview of antibiotics” for details.	Disulfiram-like reaction Metallic taste Vestibular dysfunction
Inhibition of folic acid synthesis and reduction
Sulfonamides and diaminopyrimidines (e.g., trimethoprim-sulfamethoxazole)			Shigella, Salmonella UTIs Prophylaxis of toxoplasmosis; prophylaxis and treatment of Pneumocystis jirovecii pneumonia	See “Overview of antibiotics” for details.	Megaloblastic anemia Leukopenia, granulocytopenia Hyperkalemia Sulfonamides can trigger hemolytic anemia (in G6PD-deficient patients) and hypersensitivity reactions
Antimycobacterial drugs
Rifamycins (e.g., rifampin)			Mycobacterial diseases: tuberculosis, leprosy Meningococcal prophylaxis H. influenzae type b chemoprophylaxis	See “Overview of antibiotics” for details.	Harmless red-orange discoloration of body fluids Cytochrome P450 induction Minor hepatotoxicity
Hydrazides (isoniazid)			Tuberculosis		Hepatotoxicity	Hepatotoxicity Anion gap metabolic acidosis Drug-induced lupus erythematosus Vitamin B₆ deficiency
Nicotinamides (pyrazinamide)			Tuberculosis		Hepatotoxicity	Hyperuricemia
Ethylenediamine derivates (ethambutol)			Tuberculosis Treatment of Mycobacterium avium-intracellulare infection		Optic neuropathy (↓ visual acuity, red-green color blindness) → irreversible blindness
Sulfones (dapsone)			Lepromatous and tuberculoid leprosy Pneumocystis jirovecii pneumonia		Methemoglobinemia Triggers hemolytic anemia in patients with G6PD deficiency Agranulocytosis
Others
Nitrofurans (nitrofurantoin)			Treatment and prophylaxis of acute uncomplicated UTIs	See “Overview of antibiotics” for details.	Pulmonary fibrosis Hemolytic anemia in patients with G6PD deficiency

Antifungals

Overview
Agents		Indications	Mechanism of action	Adverse effects
Polyenes (e.g., amphotericin B, nyastin)		See “Overview of antifungals and their mechanisms of action” for details.
Azoles	Triazoles (e.g., fluconazole, itraconazole)
Azoles	Imidazoles (e.g., ketoconazole, clotrimazole)
Echinocandins (e.g., caspofungin)
Pyridone derivatives (ciclopirox)
Benzofurans (griseofulvin)
Antimetabolites (flucytosine)

Antihelminthic drugs

Overview
Drug	Indications	Mechanism of action	Adverse effects
Bendazoles (e.g., albendazole, mebendazole)	See “Overview of antihelminthic agents” for details.
Pyrantel pamoate
Praziquantel
Ivermectin
Diethylcarbamazine

Antimalarial drugs

Overview
Agents	Indications	Mechanism of action	Adverse effects
Chloroquine	See “Overview of antimalarial drugs” for details.
Hydroxychloroquine
Doxycycline/tetracycline
Mefloquine
Quinine
Artemether-lumefantrine
Atovaquone-proguanil
Quinidine
Artesunate
Primaquine

Antiprotozoal drugs

Overview
Agents	Indications	Mechanism of action	Adverse effects
Pentamidine	See “Overview of antiprotozoal agents” for details.
Suramin
Eflornithine
Nifurtimox
Melarsoprol
Sodium stibogluconate
Paromomycin
Miltefosine
Diloxanide
Iodoquinol

Antivirals

Hepatitis viruses

Overview
Agents		Mechanism of action	Indications	Adverse effects
Antivirals against both hepatitis B and C
Pegylated interferon-α and interferon-α		See “Overview of antivirals against both hepatitis B and C” for details.
Antivirals against hepatitis B
Nucleotide analogs (e.g., tenofovir, adefovir)		See “Overview of antivirals against hepatitis B” for details.
Nucleoside analogs (e.g., entecavir, lamivudine)
Antivirals against hepatitis C
Guanosine analogs (e.g., ribavirin)		See “Overview of antivirals against hepatitis C” for details.
Direct-acting antivirals (DAAs)	NS3/4A protease inhibitors (e.g., simeprevir, grazoprevir)
	Nonnucleoside NS5A polymerase inhibitors (e.g., ledipasvir, ombitasvir)
	NS5B inhibitors (e.g., dasabuvir, sofosbuvir)

Herpes viruses

Overview
Agents		Indications	Mechanism of action	Adverse effects
Nucleoside analogs	Acyclovir, valacyclovir	See “Overview of antivirals against herpes viruses” for details.
	Ganciclovir, valganciclovir
	Cidofovir
Pyrophosphate analogs (e.g., foscarnet)
Antisense oligonucleotides (e.g., fomivirsen)

Influenza viruses

Overview
Agents	Indications	Mechanism of action	Adverse effects
NMDA receptor antagonists (e.g., amantadine, rimantadine)	See “Overview of antivirals against influenza viruses” for details.
Neuraminidase inhibitors (e.g., oseltamivir, zanamivir)
RNA polymerase endonuclease inhibitor (baloxavir marboxil)

Ectoparasiticides

Overview
Drug	Indications	Mechanism of action	Adverse effects
Permethrin	See “Overview of ectoparasiticides” for details.
Dimeticone
Malathion

Biologics

Overview
Agents		Indications	Mechanism of action	Adverse effects
TNF-α inhibitors	Monoclonal antibodies (e.g., infliximab, adalimumab)	See “Overview of biologics” for details.
TNF-α inhibitors	Fusion proteins (e.g., etanercept)
CD20 antibodies (e.g., rituximab)
Alpha-4 integrin antibodies (e.g, natalizumab)
CD52 antibodies (e.g., alemtuzumab)
PD-1 antibodies (e.g., pembrolizumab, nivolumab)
PD-L1 antibodies (e.g., durvalumab)
CTLA-4 antibodies (e.g., ipilimumab)
Interleukin-2 receptor alpha chain antibodies (e.g., basiliximab, daclizumab)
IgE antibodies (e.g., omalizumab)
GpIIb/IIIa inhibitors (e.g., abciximab)
CD3 antibodies (e.g., muromonab-CD3)
ERBB2 (HER2/neu) antibodies (e.g., trastuzumab)
VEGF antibodies (e.g., bevacizumab)
C5 antibodies (e.g., eculizumab)
RANKL antibodies (e.g., denosumab)
IL-12/IL-23 antibodies (e.g., ustekinumab, guselkumab)
EGFR inhibitors (e.g., cetuximab, panitumumab)
IL-6 receptor antibodies (e.g., tocilizumab)
IL-17A antibodies (e.g., secukinumab, ixekizumab) ^[6]
RSV F protein antibodies (e.g., palivizumab) ^[7]
α4β7 integrin antibodies (e.g., vedolizumab)

Cardiovascular drugs

This section provides an overview of the most important drug classes and substances targeting the cardiovascular system.

Antiarrhythmics

Overview
Agents		Indications	Mechanism of action	Adverse effects	Contraindications	Interactions
Sodium channel blockers (class I)	Class IA (e.g., quinidine, procainamide)	See “Classes of antiarrhythmic drugs” for details.			Quinidine: history of immune thrombocytopenia Procainamide: lupus erythematosus, complete heart block	Serum levels of quinidine are increased by amiodarone and cimetidine and decreased by nifedipine.
	Class IB (e.g., lidocaine, phenytoin)				Phenytoin: pregnancy Lidocaine: conduction abnormalities (e.g., WPW syndrome, intraventricular block)	Phenytoin induces cytochrome P450 Propranolol, cimetidine → ↑ lidocaine serum concentrations → toxic accumulation
	Class IC (e.g., propafenon)				Cardiogenic shock Bradycardia Electrolyte imbalances	Increases digoxin and warfarin concentrations
Beta blockers (class II; e.g., metoprolol, propranolol)					See “Contraindications to beta blockers” for details.	Nondihydropyridines: ↑ risk of AV block Cocaine: ↑ blood pressure, coronary and systemic vasoconstriction
Potassium channel blockers (class III; e.g., amiodarone) ^[8]					Sinus bradycardia Cardiogenic shock AV block	Fluoroquinolones, macrolides, azoles: ↑ risk of QTc prolongation and Torsades de pointes Various CYP450 enzyme interactions
Calcium channel blockers (class IV; diltiazem, verapamil)					Preexisting cardiac conduction disorders (e.g., WPW, bradycardia, AV block)	Beta blockers: ↑ risk of AV block
Ivabradine		Congestive heart failure (NYHA class II–III, stable HFrEF ≤ 35%, and sinus rhythm ≥ 70 bpm at rest on maximum tolerated beta-blocker dose)	Selectively inhibits I_f channel in the pacemaker cells of the SA node → prolongation of slow depolarization (phase 4) → ↓ heart rate	Vision changes: luminous phenomena (enhanced visual brightness) Bradycardia Hypertension	Decompensated heart failure Conduction abnormalities	Simultaneous treatment with CYP3A4 inhibitors/inducers should be avoided.
Adenosine		Diagnosis and termination of certain forms of paroxysmal supraventricular tachycardias (e.g., AVNRT, orthodromic AVRT) Diagnosis of underlying atrial fibrillation in supraventricular tachyarrhythmias	Activates Gi protein → inhibition of adenylate cyclase → ↓ cAMP → deactivation of L-type Ca²⁺ channels and activation of K⁺ channels → ↓ Ca²⁺ and ↑ K⁺ efflux → hyperpolarization → transient AV node block (15 seconds) → acute termination of supraventricular tachycardia	Chest pain, flushing, hypotension, bronchospasm Sense of impending doom AV block, asystole	Preexcitation syndromes: antidromic AVRT, WPW AV block Asthma	Theophylline and caffeine: ↓ adenosine effects
Magnesium sulfate ^[9]		Torsades de pointes Digoxin intoxication Eclampsia	Decreases calcium influx → prevention of early afterdepolarizations	Hypotension, asystole Drowsiness, loss of reflexes Respiratory depression	Myasthenia gravis Heart block	Dihydropyridines: hypotension Neuromuscular blocking agents: ↑ duration of blockade
Digoxin		Atrial fibrillation Chronic systolic heart failure	Inhibits Na⁺/K⁺-ATPases → ↑ contractility, ↓ heart rate	Nausea, vomiting, diarrhea Visual disturbances (blurry vision with a yellow tint and halos) Intoxication: severe arrhythmias	Ventricular fibrillation May be used with caution in pregnant women	K⁺-depleting diuretics: hypokalemia → arrhythmias Verapamil, diltiazem, amiodarone, quinidine: ↑ risk of overdose

Antihypertensives

Overview
Agents			Indications	Mechanism of action		Adverse effects		Contraindications	Interactions
First-line antihypertensives
Angiotensin-converting enzyme inhibitors (e.g., lisinopril, captopril, enalapril)			First-line drug in patients with diabetes mellitus, renal disease (nephroprotective) Heart failure with reduced ejection fraction	Inhibition of ACE → ↓ conversion of angiotensin I to angiotensin II		Dry cough, angioedema (bradykinin-mediated in ACEIs) Hyperkalemia ACEIs: pemphigus vulgaris		C1 esterase inhibitor deficiency Pregnancy Relative: bilateral renal artery stenosis, solitary kidney	Other antihypertensive drugs: ↑ hypotensive effect NSAIDs: ↓ antihypertensive effect Potassium-sparing diuretics or other drugs that increase potassium level: ↑ hyperkalemia ↑ Level of lithium
Angiotensin-receptor blockers (sartans; e.g., valsartan, candesartan)			Same as ACE inhibitors; mostly used if ACE inhibitors are not tolerated	Inhibition of angiotensin II receptor type 1
Thiazide diuretics			See “Diuretics” below for details.
Calcium channel blockers (CCBs)	Dihydropyridines (e.g., nifedipine, amlodipine) ^[10]		See “Overview of calcium channel blockers” for details.
	Nondihydropyridines	Benzothiazepines (diltiazem)
	Nondihydropyridines	Phenylalkylamines (verapamil)
Second-line antihypertensives
Beta blockers (e.g., propranolol, metoprolol, labetalol)			See “Characteristics of beta blockers” for details.	See “Overview of β-adrenergic blockade” for details.		See “Adverse effects of beta blockers” for details.		See “Contraindications to beta blockers” for details.	Nondihydropyridines: ↑ risk of AV block
Loop diuretics (e.g., furosemide, torsemide)			See “Diuretics” below for details.
Aldosterone antagonists (e.g., eplerenone, spironolactone)			See “Diuretics” below for details.
Direct renin inhibitors (e.g., aliskiren)			Arterial hypertension if both ACE inhibitors and ARBs are not tolerated	Direct inhibition of renin		Hyperkalemia Angioedema		Pregnancy Current treatment with ACE inhibitors or ARBs	P-glycoprotein inhibitors (e.g., ketoconazole, verapamil): ↑ aliskiren level
Direct arteriolar vasodilators		Hydralazine ^[11]	First-line treatment in pregnancy	Increase the release of cGMP → relaxation of smooth muscle → vasodilation → ↓ afterload	Arterioles > veins	Angina Sodium and water retention Drug-induced lupus erythematosus	Peripheral neuritis	Coronary artery disease	Other hypotensive drugs (antihypertensives, anesthetics, sedatives): ↓↓ blood pressure
Direct arteriolar vasodilators		Sodium nitroprusside ^[12]	Hypertensive emergencies		Arteries = veins		Cyanide toxicity	Decreased cerebral circulation Leber optic atrophy
Alpha-1 blockers (e.g., doxazosin, prazosin) ^[13]			See “Overview of sympatholytic drugs” for details.			See “Overview of alpha receptor antagonists” for details.		Hypersensitivity	PDE-5 inhibitors: ↓↓ blood pressure ^[14]
Alpha-2 agonists (e.g., clonidine)			See “Overview of sympatholytic drugs” for details.			See “Overview of alpha-2 receptor agonists” for details.		Severe coronary insufficiency, recent myocardial infarction	Sedatives, alcohol, barbiturates: ↑ CNS depression ^[15]

Lipid-lowering agents

Overview
Agents	Indications	Mechanism of action	Adverse effects	Contraindications	Interactions
Statins (e.g., atorvastatin, simvastatin)	See “Overview of lipid-lowering agents” for details.
Bile acid sequestrants (e.g., cholestyramine, colestipol)
Ezetimibe
Fibrates (e.g., bezafibrate, fenofibrate, gemfibrozil)
Niacin
PCSK9 inhibitors (e.g., alirocumab, evolocumab)
Marine omega-3 fatty acids (fish oil)
Lomitapide

Central and peripheral nervous system drugs

This section provides an overview of the most important drug classes and substances that act on the central and peripheral nervous system.

Anesthetics

Overview
Agents		Indications	Mechanism of action	Adverse effects
Intravenous anesthetics
Propofol		See “Overview of intravenous anesthetics” for details.
Etomidate
Ketamine
Barbiturates
Benzodiazepines
Opioids
Inhalational anesthetics
Nitrous oxide		See “Overview of inhalational anesthetics” for details.
Desflurane
Sevoflurane
Isoflurane
Enflurane
Halothane
Methoxyflurane
Local anesthetics
Ester group anesthetics	Short-acting (e.g., procaine)	See “Overview of local anesthetics” for details.
Ester group anesthetics	Long-acting (e.g., tetracaine)
Amide group anesthetics	Intermediate-acting (e.g., lidocaine)
Amide group anesthetics	Long-acting (e.g., bupivacaine)

Anticonvulsants

Overview
Agents		Indications	Mechanism of action	Adverse effects	Contraindications	Interactions
First-generation (classic) anticonvulsants	Valproate	See “Overview of first-generation anticonvulsants” for details.
	Carbamazepine
	Ethosuximide
	Phenytoin/fosphenytoin
	Phenobarbital
	Benzodiazepines
Second-generation (newer) anticonvulsants	Lamotrigine ^[16]	See “Overview of second-generation anticonvulsants” for details.
	Tiagabine ^[17]
	Levetiracetam ^[18]
	Pregabalin
	Gabapentin
	Vigabatrin ^[19]
	Topiramate ^[20]

Antidepressants and mood stabilizers

Overview
Agents		Indications	Mechanism of action	Adverse effects	Contraindications	Interactions
St. John's Wort		See “Overview of antidepressants” for details.
Selective serotonin reuptake inhibitors (SSRIs; e.g., fluoxetine, sertraline, citalopram)
Serotonin-norepinephrine reuptake inhibitors (SNRIs; e.g., venlafaxine, duloxetine)
Tricyclic antidepressants (TCAs)	Secondary amines (e.g., nortriptyline, desipramine)
Tricyclic antidepressants (TCAs)	Tertiary amines (e.g., amitriptyline, imipramine)
Serotonin antagonist and reuptake inhibitors (SARIs; e.g., trazodone)
Monoamine oxidase inhibitors (MAOIs; e.g., tranylcypromine, phenelzine, selegiline)
Atypical antidepressants	Mirtazapine
	Bupropion ^[21]
	Vilazodone
	Vortioxetine
	Varenicline
	Buspirone
Mood stabilizers
Lithium		Bipolar disorder (mood stabilization in patients with acute mania and maintenance therapy) Augmentation in treatment-resistant depression	Inhibition of the phosphoinositol cascade	Gastrointestinal upset, tremor, acne Hypothyroidism Nephrogenic diabetes insipidus Lithium toxicity	Advanced renal failure Severe cardiovascular disease Pregnancy	Thiazide diuretics, NSAIDs, ACEIs: ↑ renal absorption of lithium → ↑ risk of lithium toxicity
Anticonvulsants (e.g., sodium valproate, carbamazepine, lamotrigine)		See “Anticonvulsants” above for details.

Antiparkinson drugs

Overview
Agents		Indications	Mechanism of action	Adverse effects
Dopamine precursors (L-DOPA)		See “Overview of antiparkinson drugs” for details.
Decarboxylase inhibitors (carbidopa, benserazide)
Dopamine agonists	Nonergot (e.g., ropinirole, pramipexole, apomorphine)
Dopamine agonists	Ergot (bromocriptine)
COMT inhibitors (entacapone, tolcapone)
NMDA antagonists (amantadine)
MAO-B inhibitors (e.g., rasagiline, selegiline)
Anticholinergic drugs (muscarinic antagonists; e.g., benztropine, biperiden)

Antipsychotics

Overview
Agents		Indications	Mechanism of action	Adverse effects
First-generation antipsychotics (FGAs)	Low-potency antipsychotics (e.g., chlorpromazine)	See “Overview of indications of antipsychotics” and “Overview of antipsychotics” for details.	See “Overview of antipsychotics” for details.	See “Overview of adverse effects of antipsychotics” for details.
First-generation antipsychotics (FGAs)	High-potency antipsychotics (e.g., haloperidol, fluphenazine)
Second-generation antipsychotics (SGAs; e.g., clozapine, olanzapine, risperidone)

Glaucoma drugs

Overview
Agents		Indications	Mechanism of action	Adverse effects
Drugs that decrease the synthesis of aqueous humor
Beta blockers (e.g., timolol, betaxolol, carteolol)		See “Overview of drugs used to treat glaucoma” for details.
Alpha-1 agonists (e.g., epinephrine)
Alpha-2 agonists (e.g., apraclonidine, brimonidine)
Carbonic anhydrase inhibitors (e.g., acetazolamide)
Drugs that improve the outflow of aqueous humor
PGF2α (e.g., latanoprost, bimatoprost)		See “Overview of drugs used to treat glaucoma” for details.
Parasympathomimetics	Direct parasympathomimetics (e.g., pilocarpine, carbachol)
Parasympathomimetics	Indirect parasympathomimetics (e.g., physostigmine, echothiophate)

Muscle relaxants

Overview
Agents		Indications	Mechanism of action	Adverse effects
Parenteral muscle relaxants
Depolarizing muscle relaxants (succinylcholine)		See “Overview of NMJ blockers” for details.
Nondepolarizing muscle relaxants	Short-acting nondepolarizing muscle relaxants (e.g., mivacurium)
	Intermediate-acting nondepolarizing muscle relaxants (e.g., rocuronium, atracurium, vecuronium)
	Long-acting nondepolarizing muscle relaxants (e.g., pancuronium, tubocurarine)
Oral muscle relaxants
Tizanidine		See “Overview of oral muscle relaxants” for details.
Baclofen
Dantrolene
Cyclobenzaprine
Oral benzodiazepines (e.g., diazepam, clonazepam)

Sedative-hypnotic drugs

Overview
Agents			Indications	Mechanism of action	Adverse effects	Contraindications	Interactions
Benzodiazepines	Short-acting (e.g., midazolam, triazolam, alprazolam, oxazepam)		See “Overview of sedative-hypnotic drugs” for details.
	Intermediate-acting (e.g., temazepam, lorazepam)
	Long-acting (e.g., diazepam, clonazepam)
Benzodiazepine-like substances (Z-drugs; e.g., zolpidem, zaleplon, eszopiclone)
Barbiturates	Ultra short duration of action (e.g., thiopental)
	Short duration of action (e.g., pentobarbital)
	Intermediate duration of action (e.g., amobarbital)
	Long duration of action	Phenobarbital
	Long duration of action	Primidone
Melatonin agonists (e.g., ramelteon)
Orexin antagonists (e.g., suvorexant)

Chemotherapeutic drugs and detoxifying agents

Overview
Agents	Indications	Mechanism of action	Adverse effects
Antimetabolites
Antifolates (e.g., methotrexate, pemetrexed)	See “Overview of important antimetabolites” for details.
Pyrimidine antagonists (e.g., 5-FU, cytarabine, gemcitabine)
Purine antagonists (e.g., 6-MP, azathioprine, fludarabine)
Ribonucleotide reductase inhibitors (e.g., hydroxyurea)
Alkylating agents
Oxazaphosphorines (e.g., cyclophosphamide, ifosfamide)	See “Overview of important alkylating agents” for details.
Nitrogen mustards (e.g., chlorambucil, melphalan)
Imidazotetrazines (e.g., temozolomide)
Nitrosoureas (e.g., carmustine, lomustine)
Alkyl sulfonates (e.g., busulfan)
Hydrazines (e.g., procarbazin)
Platinum-based agents (e.g., cisplatin, oxaliplatin)
Topoisomerase inhibitors
Topoisomerase I inhibitors (e.g., irinotecan, topotecan)	See “Overview of important topoisomerase inhibitors” for details.
Topoisomerase II inhibitors (e.g., etoposide)
Mitotic inhibitors
Vinca alkaloids (e.g., vincristine, vinblastine)	See “Overview of important mitotic inhibitors” for details.
Taxanes (e.g., paclitaxel)
Nontaxane microtubule inhibitors (e.g., eribulin, ixabepilone)
Cytotoxic antibiotics
Bleomycin	See “Overview of important cytotoxic antibiotics” for details.
Actinomycin D (dactinomycin)
Anthracyclines (e.g., doxorubicin)
Mitomycin
Protein kinase inhibitors
BCR-ABL and c-KIT tyrosine kinase inhibitors (e.g., imatinib, dasatinib, nilotinib)	See “Overview of important protein kinase inhibitors” for details.
EGFR tyrosine kinase inhibitors (e.g., erlotinib, gefitinib)
ALK tyrosine kinase inhibitors (e.g., alectinib)
V600E mutated-BRAF oncogene inhibitors (e.g., dabrafenib, vemurafenib)
MEK inhibitors (e.g., trametinib)
Bruton kinase inhibitors (e.g., ibrutinib)
Janus kinase inhibitors (ruxolitinib)
CDK inhibitors (e.g., palbociclib)
Other groups
Enzymes (e.g., L-asparaginase)	See “Overview of chemotherapeutic agents from other groups” for details.
Proteasome inhibitors (e.g., carfilzomib, bortezomib)
PARP inhibitors (e.g., olaparib)
Monoclonal antibodies	See section “Biologics” above.
Detoxifying agents
Agents	Indications	Mechanism of action	Preventable adverse effect
Leucovorin	See “Overview of important detoxifying agents for antineoplastic treatment” for details.
Mesna
Amifostine
Dexrazoxane

Contraceptive methods

Overview
Agents		Indications	Mechanism of action		Adverse effects
Hormonal contraception
Oral contraceptive pill	Progestin-only contraceptive pills (POPs; minipill)	Estrogen-containing contraceptives are contraindicated	Norethindrone	Exogenous estrogen → ↓ release of GnRH and gonadotropins → inhibition of ovulation and ovarian folliculogenesis Progestin Inhibits GnRH and LH secretion → suppression of ovulation Inhibits endometrial proliferation, thereby preventing implantation of the embryo Changes cervical mucus (↓ volume and ↑ viscosity), impairs fallopian tube peristalsis → inhibition of sperm ascension and egg implantation Inhibits follicular maturation Antiprogestin inhibits progesterone receptors → inhibition or delay of ovulation, suppression of endometrial maturation, and pregnancy termination	Estrogen VTE, hypertension, cardiovascular events Hepatic adenoma Progestin: breakthrough bleeding, follicular cysts
Oral contraceptive pill	Combined oral contraceptive (COC)	Contraception Hyperandrogenism, menstrual cycle disorders, symptom control in endometriosis, leiomyomas	Estrogen and progestin
Contraceptive patch		Similar to COC	Estrogen and progestin
Vaginal ring		Similar to COC	Ethinyl estradiol and etonogestrel
Injectable progestin		Estrogen-containing contraceptives are contraindicated Individuals who may not remember or be able to use short-acting contraceptives consistently	Depot medroxyprogesterone acetate (DMPA): long-acting progestin-only contraceptive
Progestin intrauterine device			Progestin
Subdermal progestin implant			Progestin
Nonhormonal contraception
Nonhormonal intrauterine device		Emergency contraception (most effective type) Long-acting contraception Estrogen-containing contraceptives are contraindicated	Altered tubal motility → spermicidal effect and prevention of implantation		No protection from sexually transmitted infections ↑ Risk of unintended pregnancy compared to hormonal contraception, condoms, and/or surgical sterilization	Menorrhagia, dysmenorrhea, uterine perforation Ectopic pregnancy Pelvic inflammatory disease
Behavioral methods	Coitus interruptus	Individuals who prefer nonhormonal contraception	The penis is withdrawn from the vagina before ejaculation.			High risk for human error
	Fertility awareness-based methods		Avoiding sexual intercourse during the ovulation period Methods: calendar method, cervical mucus method, basal body temperature method, symptothermal method			High risk for human error
	Lactational amenorrhea		Suckling at the breast → ↑ prolactin and ↓ gonadotropin-releasing hormone → suppression of ovulation			Higher failure rate if breastfeeding is interrupted
	Vaginal douche		The vagina is flushed with water or other products immediately after male ejaculation during intercourse in an attempt to flush out semen			Likely highly unreliable
Barrier methods	Spermicides		Foams or jellies that are inserted into the vagina prior to sexual intercourse → spermicidal effects			Vaginal irritation
	Diaphragm		Dome-shaped latex, metal, or plastic device that holds spermicide is placed into the anterior and posterior fornix of the vagina prior to sexual intercourse → prevention of semen passing into the cervix			Toxic shock syndrome
	Cervical cap		Cup-shaped latex, metal, or plastic device that holds spermicide is placed over the base of the cervix → prevention of semen passing into the cervical canal			Toxic shock syndrome	Cervical erosion
	Sponge		Foam disk containing spermicidal fluid is inserted → prevention of semen entering the cervix; spermicidal effects			Toxic shock syndrome	Vaginal irritation
	Condom		A thin sheath that is placed over the shaft of the penis or in the vaginal canal prior to sexual intercourse → physical barrier between penile, vaginal, and/or anal secretions		Unintended pregnancy or infection due to breakage High risk of poor compliance
Surgical sterilization	Vasectomy	If permanent contraception is desired	Division and removal of a section of the vas deferens		Hematoma, surgical site infection No protection from sexually transmitted infections	Failure Sperm granulomas, postvasectomy pain syndrome
Surgical sterilization	Female sterilization	If permanent contraception is desired	Surgical interruption of the fallopian tubes			↑ Risk of ectopic pregnancy
Emergency contraception
Hormonal methods	Levonorgestrel	Emergency contraception	See “Overview of reproductive system drugs” for details.
	Antiprogestins (e.g., ulipristal acetate)
	Ethinyl estradiol PLUS levonorgestrel (Yuzpe regimen)
Nonhormonal methods (copper-containing intrauterine devices)			See above.

Diuretics

Overview
Agents		Indications
Osmotic agents (e.g., mannitol, urea)		See “Overview of diuretic agents” for details.
Carbonic anhydrase inhibitors (e.g., acetazolamide) ^[22]
Thiazide diuretics (e.g., hydrochlorothiazide)
Loop diuretics	Sulfonamides (e.g., furosemide) ^[23]
Loop diuretics	Ethacrynic acid ^[24]
Potassium-sparing diuretics	Aldosterone receptor antagonists (spironolactone, eplerenone) ^[25]
Potassium-sparing diuretics	Epithelial sodium channel blockers (triamterene, amiloride)

Endocrine drugs

This section provides an overview of the most important drug classes and substances targeting the endocrine system.

Antidiabetics

Overview
Agents		Indications	Mechanism of action	Adverse effects	Contraindications	Interactions
Insulinotropic antidiabetics
Sulfonylureas	First-generation (chlorpropamide, tolbutamide)	See “Overview of antidiabetic drugs” for details.
Sulfonylureas	Second-generation (glyburide, glimepiride)
Meglitinides (nateglinide, repaglinide)
Dipeptidyl peptidase-4 (DPP-4) inhibitors (e.g., saxagliptin)
Glucagon-like peptide-1 (GLP-1) receptor agonists (incretin mimetic drugs, e.g., exenatide)
Noninsulinotropic antidiabetics
Biguanides (metformin)		See “Overview of antidiabetic drugs” for details.
Sodium-glucose cotransporter 2 (SGLT-2) inhibitors (canagliflozin, dapagliflozin)
Alpha-glucosidase inhibitors (acarbose)
Thiazolidinediones (pioglitazone)
Amylin analogs (pramlintide)
Insulin ^[26]
Rapid-acting insulin (e.g., lispro, aspart, glulisine)		Type 1 diabetes mellitus Type 2 diabetes mellitus Gestational diabetes mellitus Acute hyperkalemia	See “Metabolic actions of insulin” for details.	Hypoglycemia Weight gain Lipodystrophy at the injection site Hypokalemia Allergic or hypersensitivity reactions	Hypoglycemia Hypersensitivity	See “Insulin drug interactions” for details.
Short-acting insulin (regular insulin)
Intermediate-acting insulin (NPH insulin)
Long-acting insulin (e.g., glargine, detemir, degludec)
Mixed insulin

Hypothalamic/pituitary gland drugs

Overview
Agents	Indications	Mechanism of action	Adverse effects
ADH antagonists (vaptans, e.g., tolvaptan, conivaptan)	See “Overview of hypothalamic and pituitary drugs” for details.
ADH analogs (e.g., desmopressin, terlipressin)
Oxytocin
Somatostatin analogs (e.g., octreotide)
GnRH agonists (e.g., goserelin leuprolide, nafarelin)
GnRH antagonists (e.g., degarelix)
GHRH analogs (e.g., tesamorelin)
GH receptor antagonists (e.g., pegvisomant)

Miscellaneous endocrine drugs

Overview
Agents		Indications	Mechanism of action	Adverse effects
Sevelamer		Hyperphosphatemia caused by CKD	Binds phosphate in the gut → ↓ serum phosphate → ↓ PTH	Nausea, vomiting, diarrhea, constipation, pain	Hypophosphatemia
Cinacalcet		Primary hyperparathyroidism after unsuccessful parathyroidectomy Hypercalcemia in hemodialysis patients with secondary hypoparathyroidism due to CKD Parathyroid carcinoma with hypercalcemia	Modulation of CaSR in parathyroid glands → ↑ sensitivity to Ca²⁺ → inhibition of PTH release	Nausea, vomiting, diarrhea, constipation, pain	Hypocalcemia
Cation-exchange medications	Resins (e.g., sodium polystyrene sulfonate)	Nonurgent lowering of K⁺	Release Na⁺ or Ca²⁺ ions in the gut, which are exchanged for K⁺ → ↑ enteral K⁺ elimination	Gastrointestinal upset Hypokalemia
Cation-exchange medications	Polymers (e.g., patiromer)	Nonurgent lowering of K⁺		Gastrointestinal upset Hypokalemia
Fludrocortisone		Mineralocorticoid replacement in adrenal insufficiency Postural hypotension 21-hydroxylase deficiency of congenital adrenal hyperplasia	Binds to mineralocorticoid receptors → ↓ sodium excretion, ↑ potassium excretion	Hypertension, heart failure Hypokalemia, muscle weakness Mood changes, cataracts
Demeclocycline		SIADH Bacterial infections Acne	Disruption of second messenger cascade in renal collecting ducts → ↓ ADH effect	Skin reactions Nausea, vomiting, diarrhea Nephrogenic diabetes insipidus

Reproductive system drugs

Overview
Agents		Indications	Mechanism of action	Adverse effects
Selective estrogen receptor modulators (SERMs; e.g., tamoxifen, raloxifene, clomiphene)		See “Overview of reproductive system drugs” for details.
Synthetic estrogens (e.g., ethinyl estradiol, mestranol, diethylstilbestrol)
Aromatase inhibitors (e.g., anastrozole, letrozole, exemestane)
Androgen agonists (e.g., danazol)
Antiandrogens	Finasteride
	Flutamide, bicalutamide
	Cyproterone
	Spironolactone
	Ketoconazole
Anabolic steroids (e,g., methyltestosterone)
Progestins (e.g., levonorgestrel, medroxyprogesterone)
Antiprogestins (e.g., mifepristone, ulipristal)

Thyroid drugs

Overview
Agents	Indications	Mechanism of action	Adverse effects	Contraindications	Interactions
Antithyroid drugs
Thionamides (e.g., carbimazole, propylthiouracil)	Inhibit thyroid peroxidase → blockade of iodide oxidation, organification, coupling Propylthiouracil: additionally inhibits 5'-deiodinase → ↓ peripheral conversion of T4 to T3		Pruritic rash Rarely: agranulocytosis, aplastic anemia, ANCA-associated vasculitis	Pregnancy (carbimazole and methimazole)	Warfarin: ↑ INR ^[27]
Potassium iodides (e.g., Lugol iodine)	Inhibit thyroid hormone release by interfering with proteolytic cleavage of T3 and T4 from thyroglobulin		Oral/gastric mucosal irritation Allergy/hypersensitivity	Pregnancy	No severe interactions
Hormone replacement drugs
Synthetic T4 (e.g., levothyroxine)	Hypothyroidism Myxedema	Synthetic thyroid hormones that produce the same effects as the endogenous hormones	Clinical features of hyperthyroidism (e.g., tachycardia, tremor, weight loss)	Uncorrected adrenal insufficiency Acute myocardial infarction	Estrogen: Increased dosage of synthetic T4 is necessary. Glucocorticoids: Decreased dosage of synthetic T4 is necessary.
Synthetic T3 (e.g., liothyronine)	Hypothyroidism Myxedema

Gastrointestinal drugs

Overview
Agents		Indications		Mechanism of action	Adverse effects
Gastric acid suppression medications and antacids
Proton pump inhibitors (PPIs; e.g., omeprazole, pantoprazole)		Gastroesophageal reflux disease	Combination treatment in H. pylori eradication therapy Peptic ulcer disease (gastric and duodenal ulcers)	Irreversible inhibition of H⁺/K⁺ ATPase in parietal cells → complete suppression of gastric acid secretion → ↑ stomach pH	↑ Risk of C. difficile infection Osteoporosis ↓ Absorption of iron, vitamin B₁₂, calcium, and magnesium Gastrointestinal upset
H2 antihistamines (e.g., cimetidine)			Anaphylactic shock (used in combination with H1 antihistamines) Symptomatic treatment of peptic ulcers	Competitive, reversible antagonism of histamine H2 receptors → ↓ gastric acid secretion	Almost all side effects are caused by cimetidine and include: Antiandrogenic effects (erectile dysfunction, gynecomastia, low libido in men) Headaches, dizziness, confusion
Antacids	Calcium carbonate		Symptomatic treatment of peptic ulcers	Alkalinization of gastric acid via alkaline ions	Hypokalemia	Hypercalcemia Acid rebound
	Magnesium hydroxide					Diarrhea
	Aluminum hydroxide					Constipation Hypophosphatemia Osteodystrophy
Antiemetics
Dopamine receptor antagonists (e.g., metoclopramide, prochlorperazine, domperidone)		See “Overview of antiemetics” for details.
Serotonin receptor antagonists (e.g, ondansetron, granisetron)
Neurokinin receptor antagonists (e.g., aprepitant)
Anticholinergic agents (e.g., scopolamine)
Antihistamines (e.g., dimenhydrinate)
Laxatives
Osmotic laxatives (e.g., polyethylene glycol, glycerin, lactulose)		Constipation		See “Overview of laxatives” for details.
Stimulant laxatives/secretory laxatives (e.g., senna, bisacodyl)
Emollient stool softener (e.g., docusate)
Bulk-forming laxatives (e.g., methylcellulose, psyllium husks, polycarbophil)
Miscellaneous
Octreotide		See “Overview of hypothalamic and pituitary drugs” for details.
Loperamide		Diarrhea		μ-receptor agonist → ↓ propulsive peristalsis and intestinal fluid secretion as well as ↑ sphincter tone	Constipation, vomiting, and nausea
Misoprostol		Prevention of NSAID-induced gastric ulcers Termination of intrauterine pregnancy, inducement of cervical ripening/labor		Prostaglandin E1 analog Relaxes vascular smooth muscle → vasodilation Reduces gastric acid production Stimulates production and secretion of mucous	Diarrhea
Orlistat		Weight loss in patients with obesity		Reversible inhibition of gastric and pancreatic lipase → ↓ breakdown and absorption of fat	Predominantly gastrointestinal side effects (e.g., pain, diarrhea, flatulence, malabsorption of fat-soluble vitamins)

Gout drugs

Overview
Agents		Indications	Mechanism of action		Adverse effects	Contraindications	Interactions
Acute gout flare
Glucocorticoids (e.g., prednisone)		See “Indications for glucocorticoid therapy” for details.	See “Pharmacodynamics of glucocorticoids” for details.		See “Side effects of glucocorticoid therapy” for details.	See “Contraindications for glucocorticoid therapy” for details.	Barbiturates, phenytoin, rifampin: ↓ serum concentrations of glucocorticoids
NSAIDs (e.g., naproxen)		See “Analgesics” section for details.
Colchicine		Acute gouty arthritis	Binds and stabilizes tubulin subunits → inhibition of microtubule polymerization → inhibition of urate crystal phagocytosis, neutrophil activation, migration, and degranulation		Gastrointestinal symptoms Rhabdomyolysis Polyneuropathy, CNS symptoms	Severe CKD	Increases statin concentrations
Chronic gout
Xanthine oxidase inhibitors (XOIs)	Allopurinol	Urate-lowering therapy (first-line)	Inhibition of xanthine oxidase → impaired hypoxanthine and xanthine degradation into uric acid	Competitive inhibition	Stevens-Johnson syndrome/toxic epidermal necrolysis	Presence of the HLA-B*5801 allele Previous hypersensitivity reaction	Purine analogs: bone marrow toxicity
Xanthine oxidase inhibitors (XOIs)	Febuxostat	Urate-lowering therapy (second-line)		Selective inhibition	Nausea, diarrhea Transaminitis	History of cardiovascular disease	Purine analogs: bone marrow toxicity
Uricosurics (e.g., probenecid)		Alternative to or used in combination with an XOI	Inhibition of uric acid reabsorption along renal proximal convoluted tubules → ↑ renal elimination		Urolithiasis (uric acid stones) Gastrointestinal symptoms, rash	Nephrolithiasis Moderate to severe CKD	Penicillin: inhibits secretion → ↑ serum concentration
Recombinant uricase (pegloticase)		Failure of first- and second-line medications	Catalyzes the breakdown of uric acid to allantoin		Infusion reactions, including anaphylaxis	G6PD deficiency	XOIs and uricosurics: interferes with monitoring

Hematologic drugs

Antiplatelet agents
Agents	Indications	Mechanism of action	Adverse effects	Contraindications	Interactions
Irreversible cyclooxgenase inhibitors (aspirin)	Acute coronary syndrome Ischemic stroke Primary prevention and management of ASCVD	See “Analgesics” section for details.	Reye syndrome Aspirin exacerbated respiratory disease GI upset Salicylate toxicity	Allergy Active/recent bleeding Major surgery/severe trauma Aspirin: febrile illness in individuals < 19 years of age, acute gout attack	Warfarin, NSAIDs: ↑ risk of bleeding ^[28]^[29]
P2Y12 receptor antagonists (e.g., clopidogrel, ticagrelor, ticlopidine)	Dual antiplatelet therapy (with acetylsalicylic acid) in STEMI Unstable angina/NSTEMI Before PCI Alternative to aspirin	Inhibition of P2Y12 receptor on platelets → ↓ expression of GpIIb/IIIa receptors on platelets → inhibition of platelet aggregation	Allergic reactions Hemorrhage GI upset
Glycoprotein IIb/IIIa inhibitors (abciximab, eptifibatide, tirofiban)	High-risk patients with unstable angina/NSTEMI before undergoing PCI	GpIIb/IIIa inhibitors bind to and block gpIIb/IIIa receptors on the surface of activated platelets → inhibition of platelet aggregation and thrombus formation	Acute thrombocytopenia Hemorrhage

Oral anticoagulants
Agents	Indications		Mechanism of action	Adverse effects	Contraindications		Interactions
Vitamin K antagonists (coumarins, e.g., phenprocoumon, warfarin)	Therapy and secondary prophylaxis of: Deep vein thrombosis Pulmonary embolism	Prophylaxis of thromboembolism in: Valvular atrial fibrillation Nonvalvular atrial fibrillation	Inhibition of hepatic vitamin K epoxide reductase → ↓ hepatic synthesis (recycling) of the active, reduced form of vitamin K → ↓ γ-carboxylation of glutamate residues on coagulation factors II, VII, IX, and X as well as protein C and protein S	Dose-dependent increased risk of bleeding Warfarin: warfarin-induced skin necrosis	Coagulopathies; hepatic dysfunction with impaired hepatic production of coagulation factors Acute bleeding	Pregnancy and breastfeeding	Foods rich in vitamin K (e.g., kale, spinach): decrease in anticoagulant effect Antibiotic therapy: damage to gut flora → increase in anticoagulant effect
Direct oral thrombin inhibitors (e.g., dabigatran)		Nonvalvular atrial fibrillation (increased risk of stroke)	Selective thrombin antagonism			Concurrent administration of ketoconazole, itraconazole, cyclosporine, tacrolimus, or dronedarone	Ketoconazole, itraconazole, cyclosporine, tacrolimus, dronedarone: insufficient metabolization and subsequent accumulation of either drug
Direct oral factor Xa inhibitors (e.g., apixaban, rivaroxaban) ^[30]		Nonvalvular atrial fibrillation (increased risk of stroke)	Selective and direct inhibition of factor Xa			Hypersensitivity Prosthetic heart valves	CYP3A4 and P-glycoprotein inhibitors: ↑ serum levels of apixaban

Parenteral anticoagulants
Agents	Indications	Mechanism of action	Adverse effects		Contraindications	Interactions
Unfractionated heparin (UFH	Low-dose therapy: deep vein thrombosis (DVT) prophylaxis High-dose therapy Atrial fibrillation DVT, acute arterial thrombosis Acute coronary syndrome, myocardial infarction Mechanical heart valve replacement	Indirect inhibitor of: Factor Xa: antithrombin III potentiation → inhibition of factor Xa → ↓ activation of prothrombin Thrombin (factor IIa) → ↓ fibrinogen activation → ↓ fibrin	Bleeding	Heparin-induced thrombocytopenia (HIT): risk of type 2 HIT LMWH:UFH ≈ 1:10 Osteoporosis	Hypersensitivity to heparin or pork ^[31]	Drugs that influence hemostasis: ↑ risk of bleeding
Low molecular weight heparin (LMWH; e.g., enoxaparin, dalteparin)	DVT treatment and prophylaxis Acute coronary syndrome	LMWH: binds to antithrombin III → inhibition of factor Xa			Poor renal function (CrCl < 30 mL/min)
Synthetic heparin (fondaparinux) ^[32]	Treatment and prophylaxis of venous thromboembolism	Binds to antithrombin III → selective inhibition of factor Xa		Occasionally: low platelet count	Poor renal function (CrCl < 30 mL/min) Bacterial endocarditis Hypersensitivity
Heparinoids (glycosaminoglycans, e.g., danaparoid)	Treatment and prophylaxis of venous thromboembolism	Inhibits thrombin generation by potentiating antithrombin-mediated inactivation of factor Xa		Rarely: asthma exacerbation	Hypersensitivity to heparinoids or pork products ^[33]
Direct thrombin inhibitors (e.g., argatroban, dabigatran)	Atrial fibrillation Venous thromboembolism Type 2 HIT	Directly inhibit thrombin (freely circulating and in association with clots)		Allergic reactions, fever	Hypersensitivity ^[34]

Fibrinolytics
Agents		Indications	Mechanism of action	Adverse effects	Contraindications	Interactions
Fibrin-specific agents	Tissue plasminogen activator (tPA)	STEMI (for details regarding fibrinolysis in STEMI, see “Fibrinolytic therapy in STEMI”) Ischemic stroke (for details regarding fibrinolysis in ischemic stroke, see “Reperfusion therapy for ischemic stroke”) Massive pulmonary embolism	Directly or indirectly increase the concentration of plasmin → cleavage of thrombin and fibrin	Bleeding (e.g., intracranial hemorrhage) Hypersensitivity	Active bleeding Prior intracranial hemorrhage Recent surgery Severe hypertension Known bleeding diathesis	Drugs that influence hemostasis: ↑ risk of bleeding Alteplase: Concomitant use of ACEIs increases the risk of orolingual angioedema. ^[35]
Fibrin-specific agents	Recombinant plasminogen activators (rtPAs; e.g., alteplase, reteplase)
Nonfibrin-specific agents (e.g., streptokinase, urokinase)

Immunosuppressants

Overview
Agents		Indications	Mechanism of action	Adverse effects
Glucocorticoids (e.g., prednisolone, hydrocortisone, dexamethasone)		See “Overview of immunosuppressants” for details.
Calcineurin inhibitors	Cyclosporine A
Calcineurin inhibitors	Tacrolimus
mTOR inhibitors (e.g., sirolimus, everolimus)
Purine analog (e.g., azathioprine)
IMDH/IMPDH inhibitors (e.g., mycophenolate mofetil)
Other cytostatic and antiproliferative agents (e.g., MTX, cyclophosphamide)
Protein drugs	Antibodies (e.g., basiliximab)
	Other biological proteins (e.g., etanercept)

Respiratory drugs

Overview
Agents		Indications		Mechanism of action	Adverse effects	Contraindications	Interactions
Pulmonary hypertension drugs
Endothelin receptor antagonists (e.g., bosentan, macitentan, ambrisentan) ^[36]		See “Overview of pulmonary vasodilator agents” for details.
Phosphodiesterase-5 inhibitors (e.g., sildenafil)
Prostacyclin analogs (e.g., iloprost, treprostinil)
Long-acting synthetic prostacyclins (e.g., epoprostenol) ^[37]
Asthma drugs
Beta-2 agonists	Short-acting beta-2 agonists (SABA; e.g., albuterol, terbutaline) ^[38]	See “Overview of commonly used asthma medications” for details.
Beta-2 agonists	Long-acting beta-2 agonists (LABA; e.g., salmeterol, formoterol) ^[39]
Muscarinic antagonists	Short-acting muscarinic antagonists (SAMA; e.g, ipratropium bromide)
Muscarinic antagonists	Long-acting muscarinic antagonists (LAMA; e.g., tiotropium bromide)
Leukotriene receptor antagonists (LTRAs; e.g., montelukast) ^[40]
Corticosteroids	Inhaled corticosteroids (ICS; e.g., budesonide, fluticasone, mometasone)
Corticosteroids	Oral corticosteroids (e.g., prednisone, methylprednisone)
Leukotriene pathway modifiers (e.g., zileuton) ^[41]		See “Overview of additional asthma drugs” for details.
Mast cell stabilizers (chromones, e.g., cromolyn sodium) ^[42]
Methylxanthines (e.g., theophylline)
Biologics	Anti-IgE antibodies (omalizumab) ^[43]
Biologics	IL-5 antibodies (e.g., mepolizumab, reslizumab) ^[44]
Miscellaneous respiratory drugs
H1 antihistamines	First-generation antihistamines (e.g., diphenhydramine, dimenhydrinate)	Allergy (e.g., pruritus, rhinitis	Anaphylactic shock Motion sickness, nausea	Competitive, reversible antagonism or inverse agonism of histamine H1 receptors → ↓ vascular permeability and ↓ allergic bronchial constriction	Sedation Anticholinergic effects Anti-α-adrenergic effects (e.g., postural hypotension)	Benign prostatic hyperplasia Angle-closure glaucoma	Hypnotics, sedatives: ↑ CNS depression ^[45]
H1 antihistamines	Second-generation antihistamines (e.g., loratadine, cetirizine)	Allergy (e.g., pruritus, rhinitis	Adjuvant treatment for anaphylactic shock			Childhood and pregnancy	No clinically relevant interactions ^[46]
Dextromethorphan (DXM)		Cough suppression		Weak opioid receptor agonist and NMDA receptor antagonist	See “Overview of opioid effects” for details.	Intoxication (e.g., alcohol, sedatives) Lung disease (e.g., asthma, chronic bronchitis)	Serotonergic drugs: ↑ risk of serotonin syndrome
Pseudoephedrine		Nasal congestion		Indirect general agonism and catecholamine release → ↓ hyperemia and edema, opening of nasal meatus and eustachian tubes	CNS stimulation Arrhythmias, hypertension	Diabetes mellitus Cardiovascular disease	MAOIs: hypertension

Teratogenic agents

Overview
Agents	Adverse effects	Recommended alternative drugs
Antibiotics
Tetracycline	See “Overview of antibiotics to avoid during pregnancy” for details.
Aminoglycosides (e.g., streptomycin)
Trimethoprim/sulfonamide
Chloramphenicol
Clarithromycin
Fluoroquinolones
Metronidazole
Antihypertensives
Diuretics	See “Overview of antihypertensives to avoid during pregnancy” for details.
Angiotensin-converting enzyme inhibitors
Angiotensin-receptor blockers
Atenolol
Antifungals
Azoles (e.g., ketoconazole, high-dose itraconazole and fluconazole)	See “Overview of antifungals to avoid during pregnancy” for details.
Antimetabolites (e.g., flucytosine)
Benzofurans (e.g., griseofulvin)
Antivirals
Efavirenz	See “Overview of antivirals to avoid during pregnancy” for details.
Ribavirin
Interferon α
Ribavirin PLUS interferon α
Didanosine PLUS stavudine
Nevirapine
Anticoagulants
Warfarin	See “Overview of anticoagulants to avoid during pregnancy” for details.
Phenprocoumon
Non-vitamin K oral anticoagulants (e.g., apixaban, rivaroxaban, dabigatran)
Analgesics
Nonsteroidal anti-inflammatory drugs	See “Overview of analgesics to avoid during pregnancy” for details.
Metamizole

Thionamides (e.g., methimazole, carbimazole, thiamazole)	See “Overview of thyroid agents to avoid during pregnancy” for details.
Radioiodine therapy
Antiepileptics
Valproate	See “Overview of antiepileptics to avoid during pregnancy” for details.
Carbamazepine
Phenytoin
Antiemetics
Domperidone	See “Antiemetic therapy for nausea and vomiting of pregnancy” for details.
Cannabinoids
Miscellaneous drugs
Steroids	See “Overview of other drugs to avoid during pregnancy.”
Oral antidiabetic agents
Methotrexate
Cholestyramine
Lithium
Antineoplastic drugs
Isotretinoin and vitamin A
Misoprostol
5α-reductase inhibitors
Antacids (calcium carbonate, magnesium hydroxide)
Trimethadione	Fetal trimethadione syndrome	N/A
Diethylstilbestrol	Vaginal clear cell adenocarcinoma Congenital anomalies of the Müllerian duct
Thalidomide	Thalidomide embryopathy
Recreational substances
Alcohol	Fetal alcohol syndrome	N/A
Amphetamines	Intrauterine growth restriction, low birth weight ↑ Risk of preterm labor and miscarriage Cigarettes: ADHD, conduct disorder, SIDS
Cigarettes (nicotine, carbon monoxide)
Cocaine
Opioids (e.g., heroin)	Respiratory depression Neonatal abstinence syndrome
Physical agents
Radiation	Microcephaly, growth restriction Intellectual disability Malignancy	N/A
Metal poisoning
Lead	Spontaneous abortion, stillbirth Hemangiomas, lymphangiomas, hydroceles, skin tags, undescended testes VACTERL	N/A
Mercury	Cerebellar atrophy Atrophy of the visual brain cortex Polyneuritis	N/A

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