Exam 3 Meds Flashcards
Empiric
Prophylactic
Definitive
Based on evidence- based guidelines
Infection prevention
Based on culture
Penicillin V and Penicillin G Benzathine
Penicillin
Activity
• Aerobic, gram positive organisms, including S. pneumoniae,
group A beta-hemolytic streptococci
Prevent bacterial cell wall synthesis during active
multiplication, causing cell wall death
• Bactericidal against susceptible bacteria
Caution:
History of hypersensitivity reaction
• Compatible in pregnancy and lactation • Approved in pediatrics
• Caution in renal impairment
AE: Nausea, vomiting, diarrhea, candidiasis, maculopapular rash, C. difficile, anaphylaxis (rare)
Amoxicillin and Amoxicillin/Clavulanic Acid
Penicillin
Activity
• Gram positive organisms, including S. pneumoniae, group A beta-hemolytic streptococci, enterococcus, and greater activity against gram negative bacteria
Prevent bacterial cell wall synthesis during active
multiplication, causing cell wall death
• Bactericidal against susceptible bacteria
Caution:
History of hypersensitivity reaction
• Compatible in pregnancy and lactation • Approved in pediatrics
• Caution in renal impairment
AE: Nausea, vomiting, diarrhea, candidiasis, maculopapular rash, C. difficile, anaphylaxis (rare)
Cefazolin, Cephalexin
First Generation Cephalosporins
Activity
• Gram positive cocci, including methicillin-sensitive S.
aureus and S. epidermidis, most streptococci, E. coli
Indications
• Cellulitis, uncomplicated cystitis, impetigo, group A beta-hemolytic streptococci (GABHS)
Cefuroxime, Cefprozil, Cefaclor
Second Generation Cephalosporins
Activity
• Gram positive cocci, including methicillin-sensitive S. aureus and S. epidermidis, most streptococci, E. coli; increased activity against H. influenzae
Indications
• Cellulitis, COPD acute exacerbation, acute otitis media, group A beta-hemolytic streptococci (GABHS), Lyme disease, uncomplicated UTI
Ceftriaxone, Cefdinir, Cefpodoxime
Third Generation Cephalosporins
Activity
• Gram positive cocci, including methicillin-sensitive S. aureus, S. pneumoniae, N. gonorrhoeae, H. flu, N. meningitidis, E. coli
Cephalosporins Info
Pharmacodynamics
• Prevent bacterial cell wall synthesis during
active multiplication, causing cell wall death • Bactericidal against susceptible bacteria
Adverse drug effects
• Nausea, vomiting, diarrhea, maculopapular rash, C. difficile, hypersensitivity reaction (rare), hemolytic anemia (rare), pain at injection site (ceftriaxone)
Caution and contraindications (first to third gen)
• History of hypersensitivity reactions
• Caution in patients with history of anaphylaxis or hypersensitivity reaction with penicillin allergy
• Caution in renal and hepatic impairment
• Compatible in pregnancy and lactation
• Approved in pediatrics
Vancomycin
Glycopeptides
Activity
• Gram positive organisms, including C. difficile
and Staph enterocolitis
• Bactericidal for gram positive organisms
Pharmacodynamics
• Inhibit bacterial cell wall synthesis by blocking glycopeptide polymerization through binding tightly to the D-A1a-D-A1a portion of cell wall precursor
Oral Vanc
Caution and contraindications
• Compatible in pregnancy and lactation • Approved in pediatrics
Adverse drug effects
• Bitter taste, mouth irritation, abdominal pain, nausea, fatigue, peripheral edema, headache
Clindamycin
Lincosamides
Activity
• Gram positive organisms, including S. pneumoniae, S. pyogenes, methicillin- resistant Staph aureus, P. acnes, as well as select anaerobic pathogens
Indications
• MRSA skin infection, strep pharyngitis, pelvic inflammatory disease
Pharmacodynamics
• Binds to the 50S subunit of the bacterial
ribosome and suppresses protein synthesis
Adverse drug effects
• Black box warning: colitis, C. difficile infection
• Maculopapular rash, abdominal pain, nausea, vomiting, dizziness, hypersensitivity reaction (rare), anaphylaxis (rare), agranulocytosis (rare)
Caution and contraindications • Caution with history of GI disease • Caution in hepatic impairment • Compatible in pregnancy • Caution in lactation • Approved in pediatrics though other antibiotics preferred
Azithromycin, Erythromycin, Clarithromycin
Macrolides
Activity
• Broad spectrum gram positive and gram negative coverage, including S. pneumoniae, MSSA, H. flu, Bordetella pertussis, Mycoplasma, Chlamydia, M. catarrhalis, H. pylori
Pharmacodynamics
• Bind to the 50S subunit of the bacterial ribosome and
suppresses protein synthesis
Adverse drug effects
• Nausea, vomiting, diarrhea, abdominal pain, skin rash, liver abnormalities (rare), hypersensitivity reactions (rare)
Caution and contraindications
• Risk of QT prolongation
• Avoid in patients at risk for torsades de pointes
• Caution in renal and hepatic impairment
• Compatible in pregnancy (except clarithromycin) • Compatible in lactation
• Approved in pediatrics
Doxycycline, Tetracycline
Activity
• Broad spectrum with good coverage for gram positive and gram negative bacteria, including S. aureus (including MRSA), S. pneumoniae, P. acnes, H. flu, Chlamydia, Mycoplasma Pneumniae, Rickettsia, T. pallidum, H. pylori
Pharmacodynamics
• Inhibit protein synthesis by reversibly binding
to the 30S subunit of the bacterial ribosome
Adverse drug effects
• Anorexia, nausea, vomiting, diarrhea, lightheadedness, dizziness, photosensitivity, hypertension, C. difficile (rare), severe skin reactions (rare)
Caution and contraindications
• Caution in renal and hepatic impairment • Avoid in pregnancy
• Short-term use only in lactation
• Avoid in children younger than 8 y/o
Ciprofloxacin, Levofloxacin
Fluoroquinolones
Activity
• Broad spectrum with especially good coverage for gram negative bacteria, including E. coli, H. flu, M. catarrhalis, P. aeruginosa, S. pneumonia, Mycoplasma
Pharmacodynamics
• Bactericidal through interference with enzymes required for the synthesis and repair of bacterial DNA and promote breakage of DNA strands
Adverse drug effects
• Headache, insomnia, dizziness, nausea, diarrhea, vomiting, phototoxicity, hypersensitivity reactions (rare), tendinitis (rare), tendon rupture (rare), C. difficile (rare)
Caution and contraindications
• Black box warning regarding risk of tendon
rupture and tendonitis
• Avoid in patients with myasthenia gravis
• Risk of QT prolongation
• Caution in renal and hepatic impairment
• Caution in elderly patients
• Caution in pregnancy and lactation
• Avoid in patients younger than 18 years old
Sulfamethoxazole and Trimethoprim
Sulfonamides and Trimethoprim
Activity
• Gram positive and gram negative, including E. coli, Toxoplasma gondil, Pneumocystitis jirovecii (PCP)
Indications
• UTI, including suppression, MRSA, PCP pneumonia
Pharmacodynamics
• Competitively inhibit dihydrofolate synthetase, which is necessary for the conversion of para- aminobenzoic acid (PABA) to dihydrofolic acid; inhibiting this pathway prevents folic acid synthesis which is important for some bacteria to survive
Caution and contraindications
• Avoid in patients with sulfa allergy
• Avoid in patients with G6PD
• Caution in folate deficiency
• Caution in renal impairment
• Alternative agents should be used in pregnancy and lactation
• Avoid in pediatrics younger than two months old
Nitrofurantoin
Activity
• Gram positive cocci and gram negative bacilli that
cause UTIs; UTIs are most often caused by E. coli.
Indication
• Uncomplicate urinary tract infections, including long- term suppression of UTIs
Pharmacodynamics
• Activated by bacteria to reactive intermediates that inactivate or alter bacterial ribosomes, leading to inhibition of protein synthesis, aerobic energy metabolism, DNA, RNA, and cell wall synthesis
Adverse drug effects
• Headache, nausea, rash, urine discoloration, hepatic dysfunction (rare), agranulocytosis (rare), hemolytic anemia (rare), peripheral neuropathy (rare), hypersensitivity reaction (rare)
Caution and contraindications
• Avoid if CrCl is less than 30 mL/min
• Caution if CrCl is less than 60 mL/min
• Avoid in G6PD
• Avoid in pregnancy at term (38–42 weeks)
• Avoid in lactation when infant is less than one month old
• Avoid in infants younger than one month old
Acyclovir, Famciclovir, Valacyclovir
Nucleoside Analogues
Pharmacodynamics•Interfere with DNA synthesis and inhibit viral replication
Adverse drug effects•Headache, nausea, vomiting, skin rash, elevated transaminases, nasopharyngitis, fatigue, depression
Caution and contraindications•Caution in renal impairment•Acyclovir is recommended in pregnancy and lactation•Acyclovir is best in pediatrics older than two years old
Ledipasvir/Sofosbuvir, Sofosbuvir/Velpatasvir
HCV
Pharmacodynamics•
Inhibit HCV protein necessary for viral replication
AE: Headache, fatigue, nausea, diarrhea, myalgias, pruritus
Caution and contraindications•Black box warning: hepatitis B virus reactivation•Avoid in pregnancy•Limited data in lactation
Oseltamivir,Zanamivir, Peramivir
Neuraminidase Inhibitors
Pharmacodynamics
Neuraminidase is a viral enzyme responsible for cleaving viral attachment to the host cell surface, allowing for viral circulation; inhibiting this enzyme prevents release of virus and halts the spreading of infection•Effective against influenza types A and B
Caution in pregnancy•Oseltamivir recommended in lactation•Caution in renal and hepatic impairment•Check labels for approved pediatric age•Avoid zanamivir with history of respiratory disease
AE: Headache, nausea, vomiting, anaphylaxis (rare), neuropsychiatric events (rare)
Baloxavir Marboxil
Pharmacodynamics
Dependent endonuclease inhibitor that interferes with viral RNA transcription, resulting in inhibition of influenza virus replication•Effective against influenza types A and B
AE: Diarrhea, nasopharyngitis
Caution and contraindications•Other agents recommended in pregnancy and lactation•Avoid in pediatrics younger than 12 years old
Fluconazole
Indications
Candidiasis—vaginal, oropharyngeal, esophageal
Pharmacodynamics
Interferes with fungal cytochrome P450 activity, decreasing ergosterol synthesis (principle sterol in fungal cell membrane) and inhibiting cell membrane formation
Caution and contraindications
Risk of QT prolongation•Caution in patients with arrhythmias•Caution in renal and hepatic impairment•Avoid in pregnancy•Caution in lactation•Approved in pediatrics
AE: Headache, dizziness, nausea, vomiting, diarrhea, hepatotoxicity (rare), anaphylaxis (rare), skin reactions (rare)
Itraconazole
Indications•Onychomycosis
Pharmacodynamics
Interferes with fungal cytochrome P450 activity, decreasing ergosterol synthesis (principle sterol in fungal cell membrane) and inhibiting cell membrane formation
Caution and contraindications
Risk of QT prolongation•Caution in patients with arrhythmias•Caution in renal and hepatic impairment•Avoid in pregnancy and lactation•Limited data pediatrics•Black box warning: avoid in patients with HF
AE: Headache, skin rash, edema, vomiting, diarrhea, hepatotoxicity (rare), skin reactions (rare)
Terbinafine
Indications
Onychomycosis
Pharmacodynamics
Synthetic allylamine derivative that inhibits squalene epoxidase, a key enzyme in sterol biosynthesis in fungi; results in fungal cell death
Caution and contraindications
Caution in patients with arrhythmias•Caution in renal and hepatic impairment•Avoid in pregnancy•Avoid in lactation•Approved in pediatrics
AE: Headache, depression, taste disturbance, nausea, vomiting, diarrhea, hepatotoxicity (rare), hepatic failure (rare), skin reactions (rare), ocular effects (rare)
Metronidazole
Activity
Gram positive and gram negative anaerobes including C. difficile, Bacteroides fragilis, H. pylori, T. vaginalis, Gardnerella vaginalis
Indications
C. difficile infection, bacterial vaginosis, H. pylorieradication, trichomoniasis, pelvic inflammatory disease
Pharmacodynamics
Diffuses into the organism and interacts with DNA to cause a loss of helical DNA structure and strand breakage, this results in inhibition of protein synthesis and cell death
Adverse drug effects
Nausea, abdominal pain, anorexia, dizziness, headache, metallic taste, dry mouth, dark urine, agranulocytosis (rare), CNS effects (rare)
Caution and contraindications
Caution in renal and hepatic impairment•Caution in patients with seizure disorder•Caution in pregnancy•Avoid in lactation•Approved in children, including infants•Black box warning: potentially carcinogenic
Tinidazole
Activity
Bacteroides fragilis, H. pylori, T. vaginalis, Gardnerella vaginalis
Indications
Bacterial vaginosis, H. pylorieradication(off label), trichomoniasis, urethritis
Pharmacodynamics
After diffusing into the organism, it is thought that tinidazole causes cytotoxicity by damaging DNA and preventing additional DNA synthesis
AE: Fatigue, metallic taste, nausea, anorexia, seizures (rare), peripheral neuropathy (rare), super infection (rare)
Caution and contraindications
Caution in hepatic impairment•Avoid in pregnancy and lactation•Approved in children older than 3 y/o•Black box warning: potentially carcinogenic
Topical Agents
Caused by S. aureus, S. pyogenes
Up to 5 lesions can be treated with mupirocin (Bactroban)
More than five lesions would benefit from cephalexin
Topical Agents
Caused by Candidainfections
Can treat with topical nystatin or clotrimazole
Topical options include miconazole and clotrimazole
Testosterone
Principle endogenous androgen responsible for promoting the growth and development of male sex organs and maintaining secondary sex characteristics
Testosterone, Part II
Indications
• Male (primary) hypogonadism
• Male (hypogonadotropic) hypogonadism
• Delayed male puberty
• Hormone therapy in transgender males (off-label use)
• Endometriosis and some postmenopausal symptoms in women (not FDA approved)
Signs and symptoms • Low libido • Decreased morning erections • Low bone mineral density • Gynecomastia • Small testes • Loss of body hair • Fatigue, depression, anemia, reduced muscle mass, increased fat mass
Low morning (8–10 a.m.) serum testosterone • Primary goal of testosterone therapy is to restore serum testosterone concentration to normal range • Testosterone therapy is indicated only for testosterone deficiency, not for impaired spermatogenesis
Virilization/sexualfunction
Improvedmusclestrengthandreducedfatmass
• Improves bone density
• Effectisseenwithinthreetosixmonthsof therapy, except for bone density, which isn’t until 24 months
Adverse effects • Acne • Prostatedisorders • Sleep apnea • Erythrocytosis • Recommend against testosterone use on “trial” basis in healthy, middle-aged men
Can be given gel, IM, subcutaneous
*not good to be given orally b/c its rapidly metablized
Contraindications
• Prostatecancer
• Male breast cancer
b/c prostate is responsive to testosterone- prostate will get even bigger and you have trouble peeing
• Severelowerurinarytractsymptoms
• Erythrocytosis (HCT over 50)
• Severe,untreatedsleepapnea • Uncontrolled CHF
Drug interactions
• Anticoagulants • Diabetic agents • Corticosteroids
*check levels 2-3 months after initiation, then 1/year…evaluate for prostate CA, check HCT
Finasteride (Proscar, Propecia)
5-Alpha Reductase Inhibitors
Treats BPH and male pattern baldness
Inhibits enzymes that converts testosterone to DHT (dihydrotestosterone)
Caution
• Prostate evaluation required for any increase in PSA while on medication
Leuprolide (Lupron)
GnRH Analogues
Luteinizing hormone (LH)-releasing hormone antagonists
• Creates reversible chemical orchiectomy state in males
• Creates reversible chemical oophorectomy state in females
Indications
• Advanced prostate cancer
• Advanced breast cancer
• Management of endometriosis and uterine fibroids (leiomyomata)
• Precocious puberty
• Pubertal suppression in transgender adolescents
Spironolactone
Aldosterone Antagonist, Part I
Aldosterone antagonist and inhibitor of 5- alpha-reductase
• Potassium sparing diuretic
Indications • Polycystic ovary syndrome • Acne • Hirsutism • Dosing • Orally 50–200 mg daily
Adverse effects • GI upset
• Gynecomastia
• Contraindicated in pregnancy (Category X)
Estrogen in Oral Contraception
Ethinyl estradiol: 20–35 mcg
• Metabolized in liver
• Monophasic, biphasic, triphasic
• No significant difference in contraceptive efficacy
• Start with lowest estrogen while maintaining cycle control
• Dose may be increased if breakthrough bleeding occurs
Conditions that carry unacceptable health risk • Age over 35 and smoking • Uncontrolled HTN • Venous thromboembolism • Current breast cancer • History of stroke • Cirrhosis • Migraine with aura • Ischemic heart disease or multiple risk factors
Advantages:
Highly effective contraceptive
• Rapidly reversible
• Regulate menstrual bleeding
• Decreased menstrual blood loss and dysmenorrhea
• Reduction in risk of ovarian and endometrial cancers
Drug Interactions with COCs
Metabolism is increased by any drug that increases liver microsomal enzyme activity
• Commonly includes anticonvulsants
• Efficacy of combined oral contraception (COC) is likely to be diminished if concurrently taking a drug with this effect
• CDC recommends against women on anticonvulsants taking COCs for contraception
• Rifampin is the only antibiotic proven to reduce serum EE and progestin levels
• Griseofulvin, an antifungal, has been associated with contraceptive failure, but limited data
Estrogen in Menopause, Part I
Indications
• Vasomotor symptoms
• Genitourinary symptoms
• Benefits outweigh risk for healthy, symptomatic women who are within 10 years of menopause or younger than 60 years old and do not have contraindications to treatment
• Long-term use for prevention of disease is no longer recommended
Formulations • Oral • Transdermal • Topical gels, emulsions, lotions • Intravaginal creams, tablets, rings • Consider type of estrogen and route of administration, as well as need for progestin
Systemic
• Vasomotor symptoms
• Oral or transdermal
• Oral has greater effect on liver due to first-pass effect
• Oral increases liver production of clotting factors, HDL, triglycerides, and proteins such as sex hormone-binding globulin (SHBG) and thyroxine-binding globulin (TBG)
Systemic
• Transdermal is associated with lower risk of venous thrombosis
and stroke
• Transdermal has less effect on serum lipids compared to comparable oral dose
• Transdermal is equally effective to oral for preserving bone density
Conjugated equine estrogens (CEEs): derived from pregnant mare’s urine, mostly comprised of estrone
• Synthetic conjugated estrogens: derived from plant source (soy, yams)
• Micronized 17-beta estradiol: structurally identical (bioidentical) to main product of premenopausal ovary
• Esterified estrogens: comparable serum estradiol/estrone levels to conjugated estrogen
• Ethinyl estradiol: more potent than others for MHT; therefore used in very low doses
Adverse effects • Breast soreness • Headaches • Elevated blood pressure • Exacerbation of diabetes • Cholestasis • Thromboembolic event • Endometrial hyperplasia
Contraindications
History of breast cancer
• Coronary heart disease
• Venous thromboembolic event • Stroke/TIA
• Active liver disease
• Unexplained vaginal bleeding • High risk endometrial cancer
Raloxifene (Evista)
Selective estrogen receptor modulator (SERM)
- Estrogen antagonist in breast: reduces risk of breast cancer
- Increase in thromboembolism and hot flashes
- No effect on heart disease or endometrium
Ospemifene (Osphena)
Selective estrogen receptor modulator (SERM)
Increases thickness and moisture of vaginal mucosa
• Indication
• Dyspareunia in postmenopausal females
• Vaginal dryness in postmenopausal females
• Oral 60 mg once daily
• Estrogen agonist effect in endometrium
• Potential increased risk of endometrial cancer if intact uterus
• Increased risk of stroke and DVT
Role of Progesterone
Thickens endometrium
• Stabilizes endometrium
• Thickens cervical mucous
• Relaxes smooth muscle of uterus • Thins vaginal mucosa
Progesterone in Contraception, Part I
Mechanism of action
• Thickening cervical mucus to inhibit sperm migration
• Suppress ovulation
• Lower mid-cycle peak of FSH and LH
• Slow egg movement through Fallopian tube
• Thin endometrium
Overall complication rates are low for all progestin-only methods
Implant, IUD, depo-shot
Adverse effects • Irregular breakthrough bleeding • Breast tenderness • Galactorrhea • Nausea • Contraindications • Known or suspected pregnancy • Known or suspected breast cancer • Undiagnosed abnormal uterine bleeding • Benign or malignant liver tumors, cirrhosis, acute liver disease
Gabapentin,Levetiracetam,Valproate, Zonisamide do not appear to reduce efficacy
Progestin only pills (POPs)
Progestin dose is lower than dose in COCs
• Norethindrone (Camila): continuously
• Drospirenone (Slynd): 24 active/4 inert tablets
• Norethindrone POP does not consistently suppress ovulation—approximately half of women ovulate
• Drospirenone POP suppresses ovulation, antimineralcorticoid activity
