Transcript Reproductive Health Drugs - Arkansas Tech University

Pharmacology
Nursing 3703
By Linda Self
 Pregnancy
is dynamic state with legion of
physiologic changes
 Maternal-placental-fetal circulation—
drugs readily cross placenta
 Placental transfer occurs by fifth week of
gestation
 Drugs
enter fetal circulation, are active as
fetus has low levels of albumin, thus low
drug binding
 Drugs to liver slowly metabolized due to
immaturity of liver
 Drugs excreted by kidney into amniotic
fluid where fetus swallows
 Blood-brain barrier poorly developed so
many drugs readily cross
 Can
use knowledge of maternal-fetal
circulation to deliver meds to fetus
 Examples include: digoxin for fetal
tachycardia, Synthroid for
hypothyroidism, PCN for exposure to
syphilis, corticosteroids to accelerate
surfactant production in preemies
 Give
meds only when absolutely
necessary
 Drugs chosen should be based on stage
of pregnancy and known information
 Any drugs used should be in the lowest
possible dosages
 Live viral vaccines should be avoided
due to possible harm to fetus
 Drug
teratogenicity likely to occur 1st
trimester
 2nd and 3rd trimester effects vary. May
result in growth retardation, respiratory
problems, infection, bleeding or
congenital heart problems
 Drugs
taken at any time during
pregnancy can affect baby’s brain
because brain development continues
throughout pregnancy and after birth
 Folic
acid supplementation important to
prevent neural tube defects
 All women of childbearing potential
should ingest 440-600 mcg of folic acid
from food +/or supplement
 Pregnancy, need 800mcg
 Ginger is ok for nausea
 A—studies
in pregnant women reveal no
risk
 B—animal studies reveal no risk to fetus
 C—risk unknown
 D—positive evidence harm
 X—contraindicated, risks outweigh
benefits
 Coumadin—spontaneous
abortion,
congenital anomalies. Heparin is
anticoagulant of choice in pregnancy.
 Anticonvulsants-high rate of
abnormalities. Dilantin, Tegretol,
Depakote are category D.
 NSAIDs
can cause congenital heart
abnormalities. Cat. D.
 ASA associated with bleeding. Cat. D.
 Cautious use of antihypertensives.
Methyldopa for hypertension in
pregnancy.
 May see hydralazine or labetalol in acute
situations.
 ACE
inhibitors and ARBs contraindicated.
Can cause renal defects, craniofacial
abnormalities, fetal limb abnormalities.
Ex. Enalapril, captopril, amlodipine.
 Antibiotics considered acceptable:
azithromycin, cephalosporins, penicillins,
clindamycin, erythromycin
 TCAs
Cat. D
 Some SSRIs Cat. C but studies reveal
relationship w/heart defects,
craniosynostosis, anencephaly
 Insulin is treatment of choice for
diabetics in pregnancy. Not aspart or
glargine.
 Lithium—cardiac defects, thyroid
abnormalities
 Anemias: iron
deficiency, physiologic and
megaloblastic
 Iron supplements may be appropriate if
iron deficiency anemia
 Folic acid supplementation in
megaloblastic anemia
 Constipation
secondary to decreased
peristalsis, increasing uterine weight on
intestines
 Treat with psyllium, docusate or MOM
 GERD-increased
abdominal pressure,
relaxed esophageal sphincter. Small
meals, avoid caffeine, may give Zantac if
necessary. Avoid PPIs.
 No Pepto-Bismol
 Gestational
diabetes-tested weeks 24-28
 Tx with nutrition and exercise
 If needed, best to use insulin or acarbose
(decreases digestion of CHO in gut)
 Nausea
and vomiting—crackers when
awakening
 Vitamin B6 may help
 Zofran and Reglan both Category B
 Grp
B streptococcus-do vaginal culture at
35-37 weeks. If positive, tx with
antibiotics at onset of labor until delivery.
 HIV-HAART. Goal is to achieve RNA load
<400 copies/ml.
 Tx reduces transmission to fetus by 2/3s.
 During labor, treat with IV zidovudine.
 Treat
infant of HIV+ mother with
zidovudine for 6 weeks
 Children with HIV infection, treat with
Bactrim by 4-6 weeks
 UTIs—treat asymptomatic bacteriuria to
prevent preterm deliveries, cystitis and
pyelonephritis. Macrodantin, possibly
cephalosporin or pcn.
 Abortion
is termination of pregnancy
before 20 weeks gestation
 Prostaglandins stimulate uterine
contractions—can be used to induce
abortion
 Cytotec (misoprostal) often used to tx
gastric ulcers. PO or intravaginally to
induce parturition
 Drugs
used to inhibit labor and maintain
pregnancy
 Uterine contractions between <37 weeks
with cervical changes are considered
premature
 Tocolytics may prolong pregnancy in
order to provide steroids (resp. develop.)
 Can use nifedipine, terbutaline, Indocin
 Magnesium sulfate under debate but still
used
 Oxytocin
stimulates uterine contraction
and “let-down”
 Pitocin is synthetic form of oxytocin
 May be used to induce labor and/or
control uterine bleeding after delivery or
to complete incomplete abortion
 Parenteral
opioids used to control pain
during labor and delivery
 Morphine, meperidine, fentanyl
 Meperidine less neonatal resp.
depression
 Stadol (butorphanol)
 Epidural analgesics—Duramorph,
fentanyl, morphine
 Epidural anesthetics-bupivacaine
 Ophthalmia
neonatorum can cause
blindness. Chlamydia trachomatis. EES to
each eye at birth. Also useful for GC.
 Vitamin K is administered to prevent
hemorrhagic disease. Infant has
immature liver, lack intestinal bacteria
(synthesize vitamin K). One dose of
phytonadione 0.5 to 1mg.
 Most
systemic drugs taken by mother
reach infant in breast milk
 Women with HIV should not breast feed
 Endogenous
estrogens and progesterone
synthesized from cholesterol
 Estrogen synthesis in adipose tissue may
be significant source of estrogen.
Requires a minimum body weight and fat
content (16-24%)
 Interrelationship of estrogens and
progesterone on each others receptors
 Composed
of three types
 Estradiol major estrogen
 Purpose—promotes growth in tissues r/t
reproduction and sexual characteristics
in women
 Menstrual cycle—1st half, increasing
levels of estrogens, 2nd half, estrogen and
progesterone continue to rise then stop
abruptly. Endometrium then sloughs.
 Placenta
produces large amounts of
estrogen during pregnancy
 Causes enlargement of uterus, growth of
glandular tissue in the breasts, broaden
pelvis
 Secreted
by corpus luteum
 Cause changes in second half of cycle
which provide for implantation and
nourishment of a fertilized ovum
 If ovum is fertilized, progesterone acts to
maintain pregnancy
 Corpus
luteum produces progesterone
during first weeks of gestation
 Placenta then takes over
 Progesterone prepares breasts for
lactation by promoting development of
milk-producing cells
 Synthetic progestins affect LDL and HDL
and may decrease glucose tolerance
 Act
1.
2.
3.
by:
Inhibit hypothalamic secretion of
gonadotropin releasing hormone, in
turn inhibits FSH and LH. No ovulation
thus no conception.
Produce cervical mucous that resists
penetration of sperm into reproductive
tract
Affect endometrial maturation and
reception of ova
 Component
of birth control pills and
other preparations for women 12-45
 Contraindicated in pregnancy
 Relieve vasomotor symptoms r/t
estrogen deficiency===ERT
 HRT—no unopposed estrogen
 For delayed sexual development
 DUB
 Debate is on whether benefits outweigh
risks
 Oppose
estrogen
 Suppress ovarian function in
dysmenorrhea, endometriosis,
endometrial cancer and DUB
 Debate on whether therapeutic or too
many risks
 Control
fertility and prevent pregnancy
 Contraception after “unprotected” sex
 Menstrual disorders (amenorrhea,
dysmenorrhea)
 Known
or suspected pregnancy—
teratogenic
 Thromboembolic disorders
 Cancers of breast or genital tissues
 Undiagnosed vaginal or uterine bleeding
 Fibroid tumors
 Altered liver function
 Gallbladder disease
 History
of cerebrovascular disease,
coronary artery disease,
thrombophlebitis, hypertension
 Women over 35 yo who smoke
 Family history of breast or reproductive
system cancer
 Conjugated
estrogens (synthetic)
Cenestin
 Conjugated estrogens –Premarin
 Estradiol-Estrace
 Estradiol hemihydrate—Vagifem
 Estradiol transdermal—Estraderm,
Climara, Vivelle
 Estrone—injection weekly
 Palliative
in metastatic breast cancer
(when anti-estrogens become less
effective)
 Black box warning: estrogen w or w/o
progestins increase lipids, coagulation
and possibly promotion of cancer
 With
minimal androgenic effects include:
desogestrel, norgestimate
 Intermediate androgenic activity:
norethindrone and ethynodiol
 High androgenic activity : norgestrel
 Depo-Provera
and Provera
(medroxyprogesterone)
 Megace (megestrol acetate)
 Aygestin (norethindrone acetate)
 Micronized
for oral use
 Does not have the negative lipid panel
effects
 For amenorrhea, DUB
 Oppose estrogens in women with intact
uterus
 Usually
contain a synthetic estrogen and
a synthetic progestin
 Monophasic—fixed amounts of estrogen
and progestins
 Biphasics—fixed amounts of estrogen
with varying doses of progestins
 Triphasics—varied amounts of both
estrogen and progestins
 Monophasics—Alesse, Loestrin, Ortho-
Novum, Yasmin, Yaz, Zovia, many more
 Biphasics—Mircette, Ortho-Novum
 Triphasics—Estrostep, Tri-Levlen,
Triphasil
 *(with varying levels of hormones, fewer
side effects)
 Progestin Only—Depo-Provera, OrthoEvra, others
 Implanon—progestin
only, 3 years, single
rod
 Mirena—IUD impregnated with
levonogestrol, 5 years
 Reason
for use
 Desired route
 Duration of action
 Transdermal estradiol –decreases
dosage needed, more like natural level
 Progestin component can cause acne,
weight gain, lipid levels
 Anti-seizure
medications and antibiotics
can decrease effectiveness of the OCP
 Estrogens can decrease effectiveness of
sulfonylurea antidiabetic drugs (increase
their metabolism)
 Warfarin effectiveness decreased
 Decreased Dilantin (phenytoin)
effectiveness
 Plan
B (levonorgestrel)
 Only product on market for avoidance of
pregnancy after unprotected intercourse
 Most effective within 24h and <72h
 Inhibits ovulation
 No effect on pregnancy after
implantation
 Vasomotor
?
s/s
Memory
 Bone health
 GU health
 Inability
to conceive after 12 months of
contraceptive-free intercourse
 1 in 10 couples degree of infertility
 May opt for ovulation induction by use of
Ovid (HCG choriogonadotropin alpha—
like LH) used with Pergonal
(menotropins—contains both FSH and
LH)
 Clomid
(clomiphene) is nonsteroidal
estrogen receptor modulator
 Inhibits negative feedback mechanism of
hypothalamus by competition with
receptors
 Signals hypothalamus to release
gonadotropin releasing
hormone>>>increases FSH and
LF>>promotes follicular maturation and
ovulation
 Preparation
of human gonadotropins FSH
and LH. Once follicles ripen, hCG is
administered.
 Use this drug when gonadotropin
secretion is insufficient
 Adverse effects: ovarian enlargement,
multiple births, spontaneous abortion
 Usually
produced by placenta
 Similar in action to LH
 Exogenous use induces ovulation in
owmne who have ovulatory failure
 Testosterone
primary male sex hormone
 Secreted by Leydig’s cells
 Instrumental in development of male
sexual characteristics, reproduction, and
metabolism
 Male
sexual characteristics
 Promotes stimulus for descent of testes
into the scrotum—usually after 7th month
of pregnancy
 11-13 years, surge of testosterone
 Consistent secretion until about 50
 Skin thickens, body hair, bones thicken,
laryngeal enlargement, skeletal muscle
(slows loss of N+ and amino acids)
 Synthetic
drugs with increased anabolic
activity and decreased androgenic
activity in relation to testosterone
 Used for tissue building and growth
stimulating effects
 For cryptorchidism
 Schedule III
 Indications:
 Low
testosterone levels in males (see
text)
 Muscle wasting as seen in HIV/AIDS
 Delayed puberty
 For growth stimulation
 To increase libido
 Serious
1.
2.
3.
4.
5.
6.
7.
8.
side effects:
Fluid retention
hyperglycemia
Decreased testicular function and
impotence
Liver disorders—neoplasms, cholestatic
hepatitis
HTN, elevated LDL, decreased HDL
Heart damage
Aggression, hostility, combativeness
May cause premature baldness
 Depo-testosterone
 Androgel
(testosterone gel)
 Android (methyltestosterone)
cryptorchidism
 Androderm (testosterone transdermal)
 Danazol endometriosis
 During
pregnancy
 Liver disease
 Prostate disease
 In
up to 42% of men ages 40-70 yo
 Multi-causation
 With
stimulation, acetylcholine enhances
production of nitric oxide
 Nitric oxide activates activity of
enzymes>>cGMP (vasodilatory)
 Inflow of blood increases secondary to
this relaxation
Also with secondary effect on cAMP which
contributes to an erection
 Cause
decreased catabolism of cGMP
(concentrated in genital tissue)
 Cause increasing cAMP which results in
an increase of arterial blood flow to
corpora
 DM, HTN, depression
 History
of dysfunction
 Use of testosterone is indicated for
decreased libido
 Concurrent
use of nitrates
 Concurrent use of alpha adrenergic
blocking agents like Flomax (tamsulosin),
Hytrin (terazosin)
 Cautin in those with cavernosal fibrosis,
Peyronie’s
 Viagra
(sildenafil)
 Cialis (tadalafil)
 Levitra (vardenafil)
 Adjust
doses in those over 65, in those
with renal or hepatic disease or those
taking EES, ketoconazole, cimetadine,
antiretrovirals
 SE—HA, blue vision, nasal congestion,
dyspepsia, dizziness
 Ensure is cardiovascularly fit to take med
 Yohimbe—psychoactive, aphrodisiac
 Ginseng—increases
resistance
 Multiple herbals
energy and