Exam 3 prototype drugs

Amoxicillin

DRUG CLASS: Broad-spectrum penicillin

USE: Treat otitis media, pharyngitis, tonsillitis, sinusitis, skin infections, respiratory infections, UTIs

MOA: Inhibits the enzyme in bacterial cell wall synthesis → bacteriostatic or bactericidal (depending on dose)

Amoxicillin

CONTRAINDICATIONS:

• Penicillin hypersensitivity

• Cephalosporin hypersensitivity

• CDAD

CLINICAL JUDGMENT:

• Have epinephrine available to counteract severe allergic reactions

• Advise pregnant women to take another form of birth control

• Encourage increased fluid intake

Amoxicillin

DRUG INTERACTIONS: 

• Aspirin → increased effect

• Oral anticoagulants → increased bleeding

• Acidic fruits and juices → decreased effects

Ceftriaxone

DRUG CLASS: 3rd-gen cephalosporin

USE: Treat otitis media, bacteremia, sepsis, surgical infections, prophylaxis, skin infections, respiratory infections, UTIs

MOA: Inhibit bacterial cell wall synthesis → bactericidal

Ceftriaxone

CONTRAINDICATIONS:

• Penicillin hypersensitivity, cephalosporin hypersensitivity, jaundice, premature neonates, CDAD, calcium IV coadministration, vitamin K deficiency

CLINICAL JUDGMENT:

• Ingest yogurt or acidophilus supplements to prevent superinfections

• Have epinephrine available to counteract severe allergic reactions

• Advise pregnant women to take another form of birth control

• Encourage increased fluid intake (to regulate temperature and excrete drug properly + prevent dehydration from diarrhea)

Ceftriaxone

DRUG INTERACTIONS: 

• Alcohol → disulfarim-like reactions: flushing, dizziness, headache, N/V, muscular cramps

• Anticoagulants → increased bleeding

• Loop diuretics, aminoglycosides, vancomycin → increased nephrotoxicity

Metronidazole

DRUG CLASS: Nitroimidazole, amebicide

USE: (1) Surgical infection prophylaxis (2) Treat acne, amebiasis, bacterial vaginosis, endocarditis, meningitis, trichomoniasis, bone/joint infections, skin infections, respiratory infections, GYN infections, intraabdominal infections (3) Treat H. pylori

MOA: Disrupt DNA and protein synthesis in susceptible bacteria and protozoa → bactericidal

Metronidazole

CONTRAINDICATIONS: First-semester pregnancy, breastfeeding, hematological disease

BLACK BOX WARNING: New primary malignancy (i.e. cancer)

CLINICAL JUDGMENT:

• Monitor LFTs, RFTs, platelets, Hg/Hct

• Check urine function (I&O)

• Monitor for altered LOC

Penicillin

Macrolides (erythromycin, azithromycin), lincosamides (clindamycin), oxazolidinones (linezolid) and glycopeptides (vancomycin) are antibiotic families used as substitutes for…

Azithromycin

DRUG CLASS: Antibacterial macrolide

USE: Treat bacterial conjunctivitis, whooping cough, otitis media, tonsillitis, pharyngitis, sinusitis, pelvic inflammatory disease, STIs, skin infections, respiratory infections

MOA: Inhibits bacterial protein synthesis → bacteriostatic or bactericidal

Azithromycin

CONTRAINDICATIONS: Hypersensitivity to macrolides, jaundice

CLINICAL JUDGMENT:

• Advise pts to report the onset of loose stools or diarrhea (to rule out CDAD).

• Administer antacids either 2 hrs before or after administering this medication

Vancomycin

DRUG CLASS: Glycopeptide

MOA: Inhibit bacterial cell wall synthesis

USE: *often used for severe infections

• Sepsis, MRSA, CDAD

CLINICAL JUDGMENT:

• Follow Vanco peak and trough levels

• Red-Man syndrome (infusion-related)

• STOP if hypotension and tachycardia

• Infuse slowly to prevent phlebitis

Doxycyline

DRUG CLASS: Tetracycline

USE: Treat acne, anthrax, amebiasis, bruceliosis, epididymitis, psittacosis, tularemia, plague, STIs, rickettsia, malaria prophylaxis, respiratory infection, skin infection, UTIs; effective against MRSA, sepsis, C. diff, chlamydia

MOA: Inhibits bacterial protein synthesis → bacteriostatic or bactericidal

Doxycycline

CONTRAINDICATIONS:

• Hypersensitivity, asthma, DM, pregnancy, renal/hepatic dysfunction, periodontal disease

CLINICAL JUDGMENT:

• Advise pts to use sunscreen and protective clothing during sun exposure.

• Advise women contemplating pregnancy to avoid tetracyclines

• DO NOT give to children < 8 yrs

Doxycycline

DRUG INTERACTIONS: 

• Milk products

• Antacids and iron

• Oral contraceptives

• Penicillin

Gentamicin sulfate

DRUG CLASS: Aminoglycoside

USE: Treat blepharitis, conjunctivitis, endocarditis, bacteremia, sepsis, respiratory infections, intraabdominal infections, bone/joint infections, skin infections, UTIs, meningitis

MOA: Inhibits bacterial protein synthesis → bactericidal

Gentamicin sulfate

CONTRAINDICATIONS:

• Hypersensitivity, neuromuscular disorders

CLINICAL JUDGMENT:

• Check that therapeutic drug monitoring (TDM) has been ordered for peak and trough levels.

• Check for hearing loss and renal function

• Monitor for superinfection

Gentamicin sulfate

DRUG INTERACTIONS: 

• Penicillin → decreased effectiveness

• Anticoagulants → increased action

Ciprofloxacin

DRUG CLASS: Quinolone, fluoroquinolone

USE: Treat sinusitus, plague, anthrax, typhoid fever, febrile neutropenia, STIs, prostatitis, respiratory infections, intraabdominal infections, bone/joint infections, UTIs, skin infections, corneal ulcers, bacterial conjunctivitis, otitis media/externa

MOA: Interferes w/ DNA gyrase needed to synthesize DNA → inhibits bacterial protein synthesis → bactericidal

Ciprofloxacin

CONTRAINDICATIONS: Hypersensitivity to quinolones, tendonitis

CLINICAL JUDGMENT:

• Advise pt to avoid strenuous physical activity or exercises

• Advise pt to report paresthesia (potential neuropathy)

• Advise pt to wear sunglasses, sunblock and protective clothing when in the sun

Trimethoprim-Suflamethoxazole (TMP-SMZ, “Septra”)

DRUG CLASS: Sulfonamide

USE: Treat otitis media, MRSA, respiratory infections, UTIs, traveler’s diarrhea, shigellosis

MOA: Inhibits folic acid synthesis and protein synthesis of nucleic acids → bactericidal

Trimethoprim-Suflamethoxazole (TMP-SMZ, “Septra”)

CONTRAINDICATIONS:

• Severe renal/hepatic disease, hypersensitivity

• Thrombocytopenia

• Infants

• Folate deficiency

CLINICAL JUDGMENT:

• If a pt has an allergy to one sulfonamide (or an egg allergy), they should avoid ALL sulfonamides due to cross-sensitivity

• DO NOT take antacids

• Advise pts to drink lots of fluids to prevent crystalluria and check urinalysis

• Advise pt to get CBC checked regularly and report bruising or bleeding

• Monitor for rhabdomyolysis (damaged muscle tissue releases proteins and electrolytes into the bloodstream)

Solifenacin succinate

DRUG CLASS: Urinary antimuscarinic, anticholinergic, bladder antispasmodic

USE: Treat overactive bladder and urinary incontinence

MOA: Exerts selective muscarinic receptor antagonist effect on all muscarinic receptors → depresses voluntary and involuntary bladder contractions (acts on smooth muscle), salivary gland secretion, gastric ciliary muscle and CNS

CONTRAINDICATIONS: Hypersensitivity, glaucoma, gastroparesis, GI obstruction, Hx of angioedema

Isoniazid (INH)

DRUG CLASS: Antimycobacterial (first-line antitubercular)

USE: (1) Treat active TB (2) Prophylactic measure against latent TB

MOA: Interferes w/ lipid and DNA synthesis → inhibits bacterial cell wall synthesis → bactericidal

Isoniazid (INH)

CONTRAINDICATIONS/CAUTION:

• Hepatic disease, hepatitis, jaundice, peripheral neuropathy; AUD, HIV, AIDS

CLINICAL JUDGMENT:

• Pyridoxine (vitamin B) supplementation minimizes neurotoxic side effects (peripheral neuropathy) and vitamin B deficiency

• Advise pts to avoid antacids, take 1-2 hrs before/after meals, and schedule eye exams

• Monitor LFTs

Nystatin

DRUG CLASS: Polyene antifungal (antimycotic)

USE: Treat cutaneous and mucocutaneous mycotic infections, including Candida and Trichophyton

MOA: Binds to ergosterol on fungal cell membrane → pores → loss of intracellular contents → cell death

CLINICAL JUDGMENT:

• Oral admin: swish and swallow

  • Most common use for oral thrush

• Topical admin: puff onto skin twice a day

Fluconazole

DRUG CLASS: Azole antifungal (antimycotic)

USE: Preferred for systemic fungal infections. Treat Candida infections (yeast infections) and cryptococcal meningitis

MOA: Inhibits ergosterol synthesis → increases leakage of the fungal cell membrane → death

Fluconazole

CAUTION: QT prolongation, renal or hepatic disease

CLINICAL JUDGMENT:

• Routes: oral, IV, vaginal, topical

• Advise pt to avoid alcohol

• Monitor renal and liver labs, and urinary output

Acyclovir

DRUG CLASS: Nucleotide analog antiviral

USE: (1) Treat HSV-1 and HSV-2 (2) Treat VZV (i.e. chickenpox, shingles)

MOA: Inhibit viral DNA synthesis and viral DNA chain

Acyclovir

CONTRAINDICATIONS:

• Hypersensitivity, valacyclovir, milk protein, electrolyte/fluid imbalance

CLINICAL JUDGMENT:

• Monitor CBC for leukopenia, thrombocytopenia, and low H&H

• Monitor LFTs and urinary output

• Be cautious w/ children and seizures

Chloroquine phosphate

DRUG CLASS: Antimalarial, 4-aminoquinoline antiprotozoal agent

USE: Tx and prophylaxis of uncomplicated malaria due to susceptible strains of Plasmodium, P. falciparum, P. knowlesi, P. ovale, P. malariae, and P. vivax

MOA: Concentrates in the acid vesicles of the parasite → inhibits polymerization of heme

Chloroquine phosphate

CONTRAINDICATIONS:

• Hypersensitivity

• Ocular disease (retinal and visual field damage)

CLINICAL JUDGMENT:

• Monitor LFTs, renal labs, urinary output

• Advise pts to report vision and hearing changes immediately (due to risk for ototoxicity and ocular/macular degeneration)

• Advise pt to avoid drinking due to risk of seizures and dizziness

• Avoid sun exposure

Ivermectin

DRUG CLASS: Broad-spectrum anthelmintic/antiparasitic

USE: (1) Drug of choice for strongyloidiasis (roundworm) and onchocerciasis (nematode warm) (2) Topically used for pediculosis capitis (lice)

MOA: Binds w/ chloride channels → influx of Cl- into parasitic cell → cell death

Ivermectin

CONTRAINDICATIONS:

• Hypersensitivity to drug components

• Asthma, hepatic impairment, immunosuppression

• Pregnancy

CLINICAL JUDGMENT:

• Administered topically and orally

• Explain the importance of handwashing (especially among families)

• Usually given 1-3 days to reduce side effects. Repeated doses may be necessary.

• NOT recommended w/ breastfeeding

Zidovudine (ZDV)

DRUG CLASS: Nucleoside reverse transcriptase inhibitor (NRTI)

USE: (1) Management of pts w/ HIV infection (2) Prevention of maternal-fetal HIV transmission

MOA: Inhibits viral enzymes reverse transcriptase inhibitor and thymidine kinase (which are necessary for viral HIV replication)

Zidovudine (ZDV)

CONTRAINDICATIONS: Life-threatening allergies or components of the preparation

BLACK BOX WARNING: Hepatotoxicity, lactic acidosis, myopathy, bone marrow suppression

CLINICAL JUDGMENT: Can be taken w/o food

Tenofovir disoproxil fumarate (TDF)

DRUG CLASS: Nucleotide reverse transcriptase inhibitor (NtRTI)

USE: (1) Management of pts w/ HIV infection (2) Tx of chronic Hepatitis B

MOA: Competes w/ AMP as substrate → inhibits viral enzyme reverse transcriptase (which is necessary for viral HIV replication)

Tenofovir disoproxil fumarate (TDF)

CONTRAINDICATIONS: Renal and hepatic dysfunction

BLACK BOX WARNING: Hepatitis B exacerbation, hepatotoxicity, lactic acidosis

Efavirenz (EFV)

DRUG CLASS: Non-nucleooside reverse transcriptase inhibitor (NNRTI)

USE: Tx of HIV-1 infection

MOA: Directly binds to reverse transverse transcriptase enzymes → blocks DNA polymerization

Efavirenz (EFV)

CONTRAINDICATIONS: Life-threatening allergies to medication or its components, concurrent use w/ St. John’s wort

CAUTION: Hx of mental illness or drug abuse

Atazanavir (ATV)

DRUG CLASS: Protease inhibitor

USE: Tx of HIV- 1 infection

MOA: Inhibits HIV protease → incapable of processing polyprotease precurors → immature and noninfectious HIV particles

Atazanavir (ATV)

CONTRAINDICATIONS: Life-threatening allergies to medication or its components, concurrent use w/ St. John’s wort, rifampin

CAUTION: Preexisting cardiac abnormalities (leads to EKG changes), hepatitis B or C, hemophilia A or B

Cyclosporine

DRUG CLASS: Calcineurin inhibitor (cytotoxic drug)

USE: (1) Kidney, heart and liver organ transplant rejection prophylaxis (2) RA, psoriasis, dry eye syndrome

MOA: Binds to cytoplasmic proteins → inhibits calcineurin phosphatases → inhibits T-lymphocyte proliferation → suppresses immune system

Cyclosporine

CONTRAINDICATIONS: Hypersensitivity, HTN, renal impairment, radiation therapy

BLACK BOX WARNING: Immunosuppression → malignancies and serious infection

CLINICAL JUDGMENT:

• AVOID grapefruit and grapefruit juice → increases concentration in blood

• Transplant recipients should NOT receive live vaccines

• Monitor BUN, creatinine, K+, Mg+, LFTs and lipids

• Present in breastmilk → risk of side effects in infants

Sirolimus

DRUG CLASS: mTOR inhibitor

USE: Prophylaxis of organ transplant rejection (in pts 13+)

MOA: Inhibits T-lymphocyte activation and proliferation + inhibits antibody production

Sirolimus

CONTRAINDICATIONS: Hypersensitivity

BLACK BOX WARNING: 

• Increases susceptibility to infection + development of lymphoma and other malignancies

• DO NOT USE in liver or lung transplant recipients due to increased morbidity and mortality

CLINICAL JUDGMENT:

• Assess immunization status

• Need for health teaching due to decreased immunity

• Used in pts 13 yrs and older

• Special precautions when handling

Varicella vaccine

DRUG CLASS: Vaccine

USE: (1) Prevention of chickenpox (or keeps breakthrough mild) (2) Prophylaxis if administered w/in 3-5 days of exposure

MOA: Stimulates active immunity against natural disease

Varicella vaccine

CONTRAINDICATIONS:

• Previous anaphylaxis to the vaccine or its components

• Pregnancy or possibility of pregnancy w/in 1 mo

• Presence of moderate to severe acute illness

• Active untreated TB