Drug Mechanism of Action Clinical Use Adverse Effects

Isoniazid Requires bioactivation; Primary drug for LTBI and Hepatotoxicity, peripheral
(INH) inhibits mycolic acid in combination therapy for neuropathy (preventable with
synthesis; resistance via katG active TB pyridoxine), hemolysis in G6PD
and inhA genes deficiency
Rifamycins Inhibit DNA-dependent RNA Rifampin: optional for LTBI; Rash, nephritis, cholestasis,
polymerase; resistance primary drug in thrombocytopenia, flu-like
emerges rapidly if used alone combination therapy for syndrome with intermittent dosing
active TB
Ethambutol Inhibits formation of Bacteriostatic; component Dose-dependent visual
arabinoglycan, a component of combination regimens disturbances (reversible),
of the mycobacterial cell wall for active TB headache, confusion,
hyperuricemia, peripheral neuritis
Pyrazinami Requires bioactivation to Bacteriostatic; component Polyarthralgia, hyperuricemia,
de form active pyrazinoic acid of combination regimens myalgia, rash, porphyria,
for active TB photosensitivity; avoid in pregnancy
Streptomyc Binds to S12 ribosomal Bactericidal; used in TB Ototoxicity, nephrotoxicity
in subunit, inhibiting protein when injectable drug
synthesis needed or for drug-
resistant strains

Drug Mechanism of Action Adverse Effects

Malaria
Chloroquine Prevents heme → hemozoin; Blood GI upset, rash, headache
schizonticide
Artemisinins Metabolism to toxic free radicals in GI upset
protozoa; Blood schizonticides
Mefloquine Unknown; Blood schizonticide GI upset, rash, cardiac abnormalities,
psychiatric disturbances, seizures
Primaquine Unknown; Active against liver forms of P. Blood cytopenias, hemolysis in G6PD
vivax, P. ovale, and P. jiroveci pneumonia deficiency
(PCP)
Atovaquone Disrupts mitochondrial metabolism; Used Fever, rash, GI upset
as Malarone (with proguanil) for P.
falciparum and PCP
Pyrimethamine, Inhibits folate synthesis; Mostly blood GI upset, rashes (sometimes severe),
Proguanil, schizonticides cytopenias
Fansidar
(pyrimethamine
+ sulfadoxine)
Amebiases
Metronidazole, Reactive metabolic products in organisms; Nausea, headache, paresthesias, disulfiram
Tinidazole For luminal and extraintestinal amebiasis, effect; tinidazole less toxic
giardiasis, trichomoniasis
Diloxanide Unknown; Luminal amebiasis Mild GI upset; avoid in pregnancy
Iodoquinol Unknown; Luminal amebiasis GI upset, rash, headache, iodine toxicity
Paromomycin Aminoglycoside; Luminal amebiasis and Minimal with oral use: mild GI upset
leishmaniasis
Trypanosoma
Pentamidine Unknown; For PCP, African Hypotension, injection pain, pancreatic
trypanosomiasis, leishmaniasis toxicity, thrombocytopenia, hallucinations
Melarsoprol Trivalent arsenical; enzyme inhibition; Fever, GI upset, encephalopathy, renal &
African trypanosomiasis cardiac damage
Nifurtimox Unknown; American trypanosomiasis Allergies, GI upset, CNS abnormalities
Suramin Unknown; African trypanosomiasis Rash, GI upset, neurologic dysfunction
Eflornithine Inhibits ornithine decarboxylase; African GI upset, liver abnormalities, seizures
trypanosomiasis
Sodium Inhibits glycolysis, nucleic acid Cardiac toxicity
Stibogluconate metabolism; Leishmaniasis, all forms
Drug Mechanism of Action Clinical Use Adverse Effects
Herpes
Acyclovir, Acyclovir and Valacyclovir Treatment and Oral: nausea, diarrhea,
Valacyclovir, Activated by viral thymidine kinase prophylaxis for HSV-1, headache; IV: potential
Penciclovir, (TK) to inhibit viral DNA polymerase HSV-2, and VZV renal and CNS toxicity
Famciclovir Penciclovir and Famciclovir inhibit (Acyclovir)
viral DNA polymerase without
activation
Cytomegalovirus
Ganciclovir, Viral activation to inhibit viral DNA Treatment of CMV Bone marrow
Valganciclovir polymerase infections in suppression, hepatic and
immunocompromised neurologic dysfunction
patients
Cidofovir, Inhibit viral DNA polymerase CMV infections and Nephrotoxicity, CNS
Foscarnet Cidofovir does not require viral acyclovir-resistant HSV effects, electrolyte
activation imbalance (Foscarnet)
Foscarnet inhibits reverse
transcriptase
Hepatitis
Interferon-α (IFN- IFN-α degrades viral RNA via Suppressive treatment Alopecia, myalgia,
α), Adefovir- activation of host cell RNAse for HBV depression, flu-like
dipivoxil, Adefovir, Entecavir, and syndrome (IFN-α); lactic
Entecavir, Lamivudine inhibit HBV polymerase acidosis, renal and
Lamivudine hepatic toxicity (Adefovir)
Ribavirin, Ribavirin inhibit viral RNA and Treatment of HCV, often Anemia, teratogenic
Sofosbuvir decrease GTP Sofosbuvir inhibits in combination effects (Ribavirin)
HCV RNA polymerase
Influenza
Amantadine, Block M2 proton channels  inhibit Historically for CNS effects (more with
Rimantadine viral replication influenza, now largely Amantadine)
obsolete
Oseltamivir, Inhibit neuraminidase  preventing Prophylaxis and Gastrointestinal effects
Zanamivir viral release treatment of influenza (Oseltamivir);
bronchospasm in
asthmatics (Zanamivir)
HCV
Elbasvir, NS5A inhibitor  inhibit viral HCV (Part of Headache Fatigue
Ledipasvir, replication and assembly combination regimen)
Ombitasvir,
Velpatasvir
Dasabuvir,Sofos NS5B inhibitor HCV Nause, Insomnia
buir
Grazoprevir NS3/4A inhibitor HCV Headache, fatigue, Sulfa
Paritapr allerg

Drug Mechanism of Action Adverse Effects

Nucleoside RT inhibitor
Abacavir, Didanosine, Inhibit HIV reverse transcriptase Zidovudine: Bone marrow suppression;
Emtricitabine, Lamivudine, after phosphorylation by cellular Abacavir: Hypersensitivity; Didanosine:
Stavudine, Tenofovir, enzymes; cross-resistance is Pancreatitis; Stavudine, Zalcitabine:
Zalcitabine, Zidovudine common but often incomplete Peripheral neuropathy
Non-nucleoside RT inhibitors
Delavirdine, Efavirenz, Inhibit HIV reverse transcriptase Delavirdine, Nevirapine: Rash, increased
Etravirine, Nevirapine without need for phosphorylation; liver enzymes; Efavirenz: Teratogenic
cross-resistance among NNRTIs but
not with NRTIs
Protease Inhibitors
Atazanavir, Darunavir, Inhibit viral protein processing; GI distress and diarrhea; Atazanavir:
Fosamprenavir, Indinavir, cross-resistance common among PIs Peripheral neuropathy; Amprenavir:
Nelfinavir, Ritonavir, Rash; Indinavir: Hyperbilirubinemia,
Saquinavir, Tipranavir nephrolithiasis
Entry Inhibitors
Enfuvirtide, Maraviroc Block viral fusion with cellular Enfuvirtide: Hypersensitivity; Maraviroc:
 membranes (Enfuvirtide); CCR5 Muscle/joint pain, diarrhea, increased
receptor antagonist (Maraviroc) liver enzymes
Integrase Inhibitors
Bictegravir, Dolutegravir, Block viral integrase of HIV-1 and GI upset, Headache, Rhabdomyolysis
Elvitegrav HIV-2 (Rare)

Category Drug Mechanism of Indications Adverse Effects

Action
Alkylating Cyclophosphamid Forms DNA cross- Breast cancer, Nausea, vomiting,
Agents e links, inhibiting DNA ovarian cancer, non- myelosuppression,
synthesis and Hodgkin’s alopecia, hemorrhagic
function lymphoma, CLL, cystitis
neuroblastoma
Other major Forms DNA cross- Various cancers Varies by drug
alkylating agents links, inhibiting DNA
synthesis
Platinum Cisplatin, Forms DNA cross- Various solid tumors Varies by drug
Analogs Carboplatin, links, leading to
Oxaliplatin apoptosis
Antimetabolite Methotrexate Inhibits DHFR, Breast cancer, head Mucositis, diarrhea,
s blocking synthesis of and neck cancer, myelosuppression
thymidylate and primary CNS
purine nucleotides lymphoma, bladder
cancer
6-Mercaptopurine Inhibits de novo Acute myelogenous Nausea, vomiting,
purine synthesis leukemia myelosuppression,
hepatotoxicity
5-Fluorouracil Inhibits thymidylate GI cancers, breast Nausea, mucositis,
synthase, interfering cancer, head and diarrhea,
with DNA and RNA neck cancer, myelosuppression,
synthesis hepatocellular neurotoxicity
cancer
Vinca Alkaloids Vincristine Interferes with ALL, Hodgkin’s and Neurotoxicity, peripheral
microtubule non-Hodgkin’s neuropathy, paralytic
assembly, impairing lymphoma, Wilms’ ileus, alopecia
mitosis tumor,
neuroblastoma
Other vinca Interferes with Various cancers Varies by drug
alkaloids microtubule assembly
Podophyllotoxi Etoposide Inhibits Lung cancer, non- Nausea, vomiting,
ns topoisomerase II, Hodgkin’s alopecia,
causing DNA damage lymphoma, gastric myelosuppression
cancer
Camptothecins Topotecan Inhibits Small cell lung Nausea, vomiting,
topoisomerase I, cancer, ovarian diarrhea,
leading to DNA cancer myelosuppression
damage
Taxanes Paclitaxel Interferes with Breast, lung, Nausea, vomiting,
microtubule ovarian, hypotension,
disassembly, gastroesophageal, arrhythmias,
impairing mitosis prostate, bladder, hypersensitivity
head and neck
cancers
Anthracyclines Doxorubicin Generates oxygen Lymphomas, Nausea, arrhythmias,
free radicals, myelomas, alopecia,
intercalates into DNA, sarcomas, breast, cardiomyopathy,
inhibits lung, ovarian, myelosuppression
topoisomerase II thyroid cancers
Tyrosine Imatinib Inhibits bcr-abl Chronic Nausea, vomiting, fluid
Kinase tyrosine kinase and myelogenous retention, diarrhea,
Inhibitors other receptor leukemia, heart failure
tyrosine kinases gastrointestinal
stromal tumor
Growth Factor Trastuzumab Inhibits HER-2/neu HER-2/neu receptor- Nausea, vomiting, chills,
Receptor receptor, blocking positive breast fever, headache, cardiac
Inhibitors EGF binding cancer dysfunction
VEGF Bevacizumab Inhibits VEGF binding, Colorectal, breast, Hypertension, infusion
Inhibitors reducing tumor non-small cell lung, reaction, arterial
vascularization and renal cancer thromboembolic events
Proteasome Bortezomib Reversibly inhibits Multiple myeloma Hypotension, edema, GI
Inhibitors chymotrypsin-like upset, peripheral
activity of 26S neuropathy, cardiac
proteasome dysfunction
Hormone Prednisone Anti-inflammatory Various (refer to Weight gain, fluid
Agonists and specific hormone retention, osteoporosis,
immunosuppressive agonist section) hyperglycemia,
effects (see Chapter infections, mood
39) changes, and adrenal
suppression with long-
term

Drug Mechanism of Action Indications Side Effects

Cyclosporine Inhibits calcineurin by Organ transplantation, Renal dysfunction, hypertension,
binding to cyclophilin graft-versus-host disease, neurotoxicity, drug-drug
autoimmune diseases interactions
Tacrolimus Inhibits calcineurin by Similar to cyclosporine Renal dysfunction, hypertension,
binding to FK506 neurotoxicity
immunophilin
Sirolimus Inhibits IL-2 signaling by Organ transplantation, Hypertriglyceridemia,
binding to cyclophilin some autoimmune hepatotoxicity, diarrhea,
diseases myelosuppression
Everolimus & Similar to sirolimus, Similar to sirolimus Hypertriglyceridemia,
Temsirolimus inhibits IL-2 signaling hepatotoxicity, diarrhea,
myelosuppression
Mycophenolate Inhibits inosine Organ transplantation, Gastrointestinal disturbances,
Mofetil monophosphate graft-versus-host disease, myelosuppression
dehydrogenase, blocking autoimmune diseases
de novo GTP synthesis
Thalidomide Complex immune effects Erythema nodosum Teratogen, somnolence, peripheral
including reduction in leprosum, multiple neuropathy, neutropenia
TNF-α production myeloma
Lenalidomide Thalidomide analog, Multiple myeloma Teratogen, somnolence, peripheral
used in multiple neuropathy, neutropenia
myeloma
Alefacept Binds to T-cell CD2 Psoriasis Reduced T-cell count,
receptor and blocks its hepatotoxicity, hypersensitivity
association with LFA-3 reaction, infection, malignancy
Antithymocyte Binds to T cells and Transplantation Hypersensitivity reaction, injection
Globulin triggers complement- site reaction, malignancy
based cytotoxicity
Antilymphocyt Similar to antithymocyte Transplantation Hypersensitivity reaction, injection
e Globulin globulin site reaction, malignancy
Immune Pooled IgG Immunoglobulin Hypersensitivity reactions, fever,
Globulin IV immunoglobulin deficiencies, autoimmune headache, chills
(IGIV) preparation from healthy disorders
donors
Anti-Rho(D) Prevents Rh sensitization Administered to Rh- Injection-site reactions, hemolysis if
Antibody by binding to Rho(D) negative mothers carrying given to Rh-positive person
(RhoGAM) antigens a Rh-positive fetus 24–72
hours after delivery
Daclizumab MAb that blocks T-cell IL- Renal transplantation Hypersensitivity reactions,
2 receptor infection, malignancy
Basiliximab Chimeric MAb similar to Renal transplantation Hypersensitivity reactions,
 daclizumab infection, malignancy
Aldesleukin Activates IL-2 receptors Renal cell carcinoma, Capillary leak syndrome,
on T, B, and NK cells melanoma exacerbation of
inflammatory/autoimmune
diseases, hypersensitivity reactions
Infliximab MAb binds to TNF-α and Inflammatory bowel Hypersensitivity reactions,
Adalimumab prevents activation of disease, rheumatoid infection, malignancy, reactivation
Etanercept TNF-α receptor arthritis, ankylosing of latent TB
Golimumab spondylitis, psoriatic
arthritis
Interferon-α- Enhances immune Leukemia, melanoma, Flu-like symptoms, fatigue,
2a responses by activating hepatitis B and C hepatotoxicity, myelosuppression,
IFN-α receptors depression, neuropsychiatric effects
Interferon-α- Used for multiple Multiple sclerosis Flu-like symptoms, fatigue,
1b sclerosis hepatotoxicity, myelosuppression,
depression, neuropsychiatric effects
Interferon-γ- Used for chronic Chronic granulomatous Flu-like symptoms, fatigue,
1b granulomatous disease disease hepatotoxicity, myelosuppression,
depression, neuropsychiatric effects

Class Drug Mechanism of Action Indications Side Effects

Short-acting β Albuterol Beta2-selective agonist, Asthma acute Tremor, tachycardia
Agonists bronchodilation attack relief (drug
of choice, not for
prophylaxis)
Metaproterenol, Similar to albuterol; Asthma acute Tremor, tachycardia
Terbutaline terbutaline also available attack relief
in oral and parenteral
forms
Long-acting β Salmeterol, Beta2-selective agonists, Asthma Tremor, tachycardia,
Agonists Formoterol, bronchodilation, prophylaxis (not cardiovascular
Indacaterol, potentiation of for acute relief), events
Vilanterol corticosteroid action COPD (for
indacaterol and
vilanterol)
Nonselective Epinephrine, Nonselective β Asthma (obsolete) Excess
Sympathomimeti Isoproterenol activation; epinephrine sympathomimetic
cs also an α agonist effect (Chapter 9)
Indirect-acting Ephedrine Releases stored Asthma (obsolete) Insomnia, tremor,
Sympathomimeti catecholamines, anorexia,
c nonselective arrhythmias
sympathetic effects
Methylxanthines Theophylline Phosphodiesterase Asthma, Insomnia, tremor,
inhibition, adenosine especially anorexia, seizures,
receptor antagonist prophylaxis arrhythmias
against nocturnal
attacks
Roflumilast Nonpurine molecule COPD Minimal
similar to theophylline,
more selective for PDE4
Caffeine Similar to theophylline, Not used in Minimal
increased CNS effect asthma or COPD
Theobromine Similar to theophylline, Not used in Minimal
increased cardiac effect asthma or COPD
Antimuscarinic Ipratropium, Competitive muscarinic Asthma and Dry mouth, cough
Agents Tiotropium, antagonists; unknown chronic
Aclidinium mechanism, possibly obstructive
 mast cell stabilizers pulmonary
disease
Mast Cell Cromolyn, Reduce release of Rarely used for Cough
Stabilizers Nedocromil inflammatory and asthma
bronchoconstrictor prophylaxis;
mediators from cromolyn used for
sensitized mast cells other applications
Leukotriene Montelukast, Pharmacologic Prophylaxis of Minimal
Antagonists Zafirlukast antagonists at LTD4 asthma
receptors
Zileuton Inhibitor of lipoxygenase, Prophylaxis of Elevation of liver
reduces synthesis of asthma enzymes
leukotrienes
Corticosteroids Beclomethasone Inhibition of Prophylaxis of Pharyngeal
phospholipase A2, asthma (inhaled) candidiasis, minimal
reduces expression of systemic steroid
cyclooxygenase toxicity
Prednisone Similar to inhaled Treatment of Systemic steroid
corticosteroids, systemic severe chronic toxicity (e.g.,
action asthma, status adrenal
asthmaticus suppression)
(parenteral)
Prednisolone Parenteral form of Similar to Systemic steroid
prednisone, used for prednisone toxicity (e.g.,
status asthmaticus adrenal
suppression)
Antibodies Omalizumab Binds IgE antibodies on Prophylaxis of Extremely
mast cells, reduces severe, refractory expensive, long-
reaction to inhaled asthma term toxicity not
antigen well documented