Medications r/t Female/Male/ Urinary Reproductive System MOA and Uses

Sex Hormones

• Used to replace hormones that are missing (surgery, menopause, etc.)

• Act to control mechanisms of the endocrine system of the body

• Sex hormones include estrogens and progestins (progesterone), most commonly in combination

• Adults taking sex hormones should receive annual medical examination, including breast exam and pap smear for females, to monitor for adverse effects

• People taking estrogens should NOT smoke because of increased risk of clots

• Hormone replacement therapy (HRT) is no longer used commonly for long term menopause patients. May be used short term for symptom management – stop as soon as possible (Increases risk of breast CA, CV events, and dementia). Topical is safer.

Sex hormones

Estrogens – conjugated equine estrogens

• Estrogens are used in to replace hormones lost at menopause, for female hypogonadism and ovarian failure, to prevent postpartum breast engorgement, for acne, to slow bone loss in osteoporosis, in combination with other hormones for contraceptives, acne relief, treat some cancers

• Conjugated estrogens are PO; other estrogens can be given as skin implants (Nexaplon), given transdermally, intravaginally, and IM

• Estrogens are responsible for secondary sex characteristics, release of FSH, LH, and proliferation of endometrial lining. Help preserve calcium and promote bone formation.

• Reductions in estrogen causes s/s of menopause

Sex hormones

Progesterone- medroxyprogesterone

• Used as contraceptives, usually in combination with estrogens.

  • Progestin-only “mini pill” for those with side effects from other forms of BCPs or if breastfeeding. Safer for women over 35, those who smoke, have HTN.

  • “Depo-Provera” – long term, injectable birth control, given every 3 months

• Progestins are also used for amenorrhea/dysmenorrhea and as part of fertility programs. Some (rare) used for emergency contraceptives. Endometriosis, cancer treatments.

  • Medroxyprogesterone is “Provera”: given for 5-10 days then stopped; should bleed in 3-7 days

• Inhibit secretion of FSH and LH, prevent follicle maturation and ovulation, inhibit uterine contraction

• Oral, IM, SubQ, transdermal, intravaginal

• Atypical off-label uses: To reduce sex drive in men, to treat BPH, improve appetite in cancer patients, feminizing HRT, treat hirsutism, reduces frequency of seizures, improve blood parameters of sickle cell

Sex hormones

Estrogen-Progesterone Combinations

• Contain estrogen and progestin – combination oral contraceptives (OCs)

  • MANY more routes – patches, vaginal ring, IM injection, implants, hormonal IUDs (focus here is on Ocs)

• Prevent pregnancy by prevention ovulation, thickening cervical mucous

• Used for contraception, reducing menstrual blood loss

Sex Hormones

Emergency Oral Contraceptives - progestin with levonorgestrel

• Plan B, One-Step, Her Style, My Choice, New Day, etc.

  • Prevent fertilization by inhibition of ovulation and thickening of cervical mucus

• Concern:

  • American College of Obstetricians and Gynecologists: “Morning-after pills do not cause an abortion. They only work if you are not already pregnant. They must be taken soon after you have sex to be effective.”

  • International Federation of Gynecology and Obstetrics (FIGO) "review of the evidence suggests that LNG [levonorgestreol] ECPs cannot prevent implantation of a fertilized egg.”

• All studies are not 100% clear, so there has been some continued discussion and legal proceedings

• Oral – Take one 1.5 mg tablet as soon as possible within 72 hours of unprotected sexual intercourse or known or suspected contraceptive failure. Some brands may have second dose after

  • Some brands are “moderately effective” if used within 5 days.

Medications Affecting Labor and Delivery

Uterine Stimulants - oxytocin

• (Pitocin or “pit”)

• Drug for “uterine motility” – stimulates contractions, assists labor, induces labor (initiates or improves)

• Acts like hypothalamic hormone oxytocin; affects neuroreceptor sites to stimulate contractions of the uterus, also stimulates milk ejection when lactating

  • Prevention and treatment of uterine atony after delivery – prevents postpartum hemorrhage

• IV and IM in labor and delivery; intranasal for milk letdown

Medications Affecting Labor and Delivery

Tocolytic Medications - terbutaline

• Calm or slow uterine contractions, prevent preterm delivery

  • Relax uterine smooth muscle

• Beta2 selective adrenergic agonist, used off label to relax uterus and prolong pregnancy

• Short term, emergency use only due to risk for serious heart arrhythmias and maternal death

• IV primarily (infusion, will increase or decrease depending on contractions). Available subQ.

• Bronchodilator for breathing

• Terminates urterin contractions (tocolytic agent) stops premature labor

• asthmatic patient on a new drug + develops muscles temors= think terbutaline

Hormone Replacement

Androgens- testosterone

• Androgens are male sex hormones, and include testosterone, which is the primary natural androgen

• Class III controlled substance – potential for misuse

• Used for replacement in hypogonadism, delayed puberty in male patients, treatment of some breast cancers

  • For “low T” – fatigue, loss of hair, depression, weakness, decreased sexual performance, decreased energy

• Available in many forms – deep injection, buccal systems, topical gels and sprays, implantable pellets, dermal patches

Drugs that block Testosterone Production

Alpha reductase inhibitor- finasteride

• Blocks testosterone production. Used for long-term BPH & prevention of male-pattern baldness.

  • By reducing usable testosterone, can reduce prostate size and increase hair growth

• PO

• Finasteride has no indications for female patients, are contraindicated in females because of androgen effects.

  • Risk for absorption through skin – do not touch tablets

Erectile Dysfunction

Phosphodiesterase type 5 Inhibitor- sildenafil

• aka Viagra

• Indicated for the treatment of erectile dysfunction, timed in coordination with the onset of sexual activity.

• Relaxes smooth muscle and causes less resistance and pressure in pulmonary bed to treat pulmonary hypertension

• Take 1 hour before anticipated sexual stimulation

Anti-infective- nitrofurnatoin

• (aka Macrobid, Macrodantin) primary in US. Also trimethoprim-sulfamethoxazole (Bactrim)

• Treats susceptible gram-positive and gram-negative pathogens

• Oral, absorption enhanced when taken with food

Urinary Rentention

Alpha-1 adrenergic antagonists- tamsulosin

• Alpha-1 adrenergic blocker, block receptors which results in dilation of arterioles, veins, relaxation of bladder and urinary tract

• Used for BPH (off label for urinary retention, lower urinary tract symptoms, kidney stone expulsion)

• Cause decrease in vascular tone, vasodilation, reduced BP

• Also block smooth muscle receptors in prostate, urethra, and bladder

• PO

Urinary Analgesic- phenazopyridine

• Is actually a dye. Used to alleviate symptoms of dysuria, burning sensations, urgency, frequency, and pain related to urinary tract irritation (from infection, trauma, etc.)

• Oral

• Symptom relief but it is NOT an antibiotic

Urinary Antispasmodic

Anticholinergic- oxybutynin

• Used as urinary tract antispasmodic, block spasms of urinary tract due to inflammation, cystitis, prostatitis.

  • Spasms can lead to dysuria, urgency, incontinence, nocturia

  • Block parasympathetic activity, suppresses bladder overactivity,  leads to relaxation of bladder and urinary tract muscles

• Available as tablets, transdermal patch, gel