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244 Cards in this Set
- Front
- Back
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Birth Control
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Interfering with the reproductive process at any step from gametogenesis to nidation
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Nidation
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implantation of a fertilized ovuum
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Effectiveness of Birth control
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expressed in terms of accidental pregnacies
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non-pharmalogic birth control methods
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surgical sterilization
mechanical devices avoiding intercourse during fertilization |
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Menstrual cycle
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follicular phase (1-14)
luteal phase (second half) full cycle typically 28 days coordinating ovarian and uterine events |
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Uterine changes
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brought about under the influence of estrogens and progesterone
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regulation of the menstrual cycle
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anterior pituitary hormones
follicule-stimulating hormone (FSH) luteinizing hormone (LH) |
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Estrogens -
biosynthesis and Elimination |
ovary is the principle organ
major estrogen produced is estradiol |
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hormones during follicular phase
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estrogen is synthesized by ovarian follicles
first half of cycle |
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hormones during luteal phase
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estrogen is synthesized by corpus leuteum
second half of cycle |
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hormones during pregnancy
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estrogen is produced by placenta
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hormones in males
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esstradiol and estrone care converted by testosterone
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major estrogen produced
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estradiol
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physiologic and pharmacologic effects of estrogens
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effects on primary and secondary sex characteristics of females
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estrogens - metabolic actions
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important effects on
bone blood vessels heart liver and CNS Positive effect on bone mass favorable effects on cholesterol |
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estrogens - ADEs
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potential for endometerial Ca
hyperplasia endometrial cancer breast cancer ovarian cancer risks to fetus for Ca and developmental abnromalities less serious problems of nausea and GI disturbances increased risk for gallbladder disease livery dysfunction CNS effects headache, dizziness, depression risk for pulmonary embolism |
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estrogens - Indications
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hormone replacement therapy after menapause
female hypogonadism acne |
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Estrogens - routes of Admin
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Oral
IV IM Intravaginal Transdermal |
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Selective Estrogen Receptor Modulators (SERMS)
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stimulates some estrogen receptors and blocks estrogen receptors selectively
developed for estrogen benefits without drawbacks ie. Tamoxifen [Nolvadex] Raloxifen [Evista] |
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Tamoxifen [Nalvadex]
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SERMs
Activates estrogen Breast cancer treatment protects against osteoporosis produces hot flashes risk of endometrial Ca and hypogonadism |
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Raloxifene [Evista]
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SERMs
does not activate estrogen protects against breast cancer and osteoporosis promotes thromboembolism induces hot flashes |
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Progestins
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have actions like progesterone
which act to gestation to prepare uterus for implantation of fertilized ovum and help maintain uterus throughout pregnancy |
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Progestins - Biosynthesis
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produced by ovaries and placenta during second half of menstrual cycle
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Progestins -
physiologic and pharmacologic effects |
effects on the endometrium and endocervical glands
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Progestins -
effects during pregnancy |
other effects --
pharmacologic doses supress release of LH and FSH |
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Progestins -
**adverse effects** |
teratogenic effects
gynecologic effects of breakthough bleeding, spotting and amenorrhea along with breat tenderness and alteration of cervical secretions have been assoc with depression jaundice edema lethargy photosensitivity nausea bloating exacerbation of acute intermittent porphyria appear to increase the risk for breast cancer from estrogens |
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progestins -
**indications** |
hormone replacement therapy
after menopause to counteract adverse effects of estrogen on the endometrium dysfunctional uterine bleeding amenorrhea endometriuosis endometrial carcinoma hyperplasia premenstrual sydrome |
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Progestins
**preps and routes** |
Oral
IM topical (intravaginal, transdermal) |
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Progestins
education |
before initiating the patient must have a PAP smear, breast exam and pevlic exam
pt must report any episodes of abnormal vaginal bleeding |
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Menopausal Hormone Therapy
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production of ovarian estrogens decreases gradually
loss of estrogen has multiple physiologic consequences: vasomotor symptoms (hot flashes) accelerated bone loss increased risk for CHD new information about breast cancer disturbing Benefits and risks *Landmark Studies: WHI and HERS** |
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Benefits of Hormone Replacement Therapy
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Suppression of vasomotor symptoms
prevention of osteoporosis possible protection against CHD helps aintain estrogen dependent tissue such as vaginal epithelium prevention of urogenital atrophy |
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Benefits of menopausal hormone therapy
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primary benefits are
suppression of vasomotor symptoms prevention of urogenital atrophy prevention of osteoporosis and related fractures prevention of colorectal cancer improved quality of life |
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datat from HERS and HERS II
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hormone therapy does NOT protect against CV disease
other benefits include: positive effect on wound healing tooth retention glycemic control |
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Harms of Hormone Therapy
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Minor ADEs includ:
fluid retention weight gain breast tenderness |
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Date from WHI
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Both ET and EPT increase risk for MI, stroke, pulmonary embolism, and DVT
increased risk for endometrial cancer (but only when used alone) risk for breast cancer, ovarian cancer, gall bladder disease, alzheimer's disease, worsens urinary incontenence |
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Recommendations on HRT use:
3 approved indications |
1) treatment of moderate to severe vasomotor symptoms assoc with menopause
2) treatment of moderate to severe symptoms of vulvar and vaginal atrophy assoc with menopause 3) prevention of postmenopausal osteoporosis |
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Oral contraceptives
Mechanism |
decrease fertilization by inhibiting ovulation
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oral contraceptives
classification |
1. combination oral contraceptives (OCs)
estrogen and progestin 2. progestin-only OCs |
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Three major subgroups of combination oral contraceptives
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monophasic
biphasic triphasic |
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oral contraception
mechanism of action |
decrease fertility by inhibiting ovulation
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oral contraception
ADEs |
risks of OCs low in comparison to risks of pregnancy
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oral contraception
effectiveness |
neary 100% effective
effectivness reduced: in overweight females if not taken regularly |
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Conbination oral contraceptives --
Adverse Effects |
thromboembolic disorders
hypertension cancer teratogenic effects abnormal uterine bleeding benign hepatic adenoma multiple births glucose tolerance |
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Combination oral contraceptives --
Contraindications |
during pregnancy
history thrombophlebitis thromboembolic disorder CVA CAD Breast Carcinoma Estrogen-dependent neoplasm bleeding disorder avoided in women >35 and diabetics |
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Oral contraceptives --
educate |
against smoking
stop 4 weeks before surgery do not increase the risk of breast cancer antibiotics decrease the effectiveness and backup method should be used if does is missed take 1 next morning and 1 next evening, and then resume even in regular menstrual cycles, contraception should be used to prevent pregancy |
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Oral contraceptives
and antibiotics |
antibiotics decrease the effectiveness and backup method should be used
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oral contraceptives - missed dose
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if dose is missed, take 1 next morning, and 1 next evening,
then return to normal |
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Combination oral contraceptives --
non-contraceptive benefits |
decreased risk of:
ovarian ca endometrial ca ovarian cysts PID PMS Fibrocystic breast disease toxic shock syndrome anemia favorable effects: relief from menstrual cramping acne |
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Combination oral contraceptives --
drug interactions redce the effects of OCs |
Refampin
Ritonavir Troglitazone Antiepileptic drugs tetracycline Ampicillin St John's wort |
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combination oral contraceptives - drug interactions
drugs whose effects are reduced by OCs |
warfarin
insulin |
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combination oral contraceptives -- drug interactions
drugs whose effects are incrased by OCs |
theophylline
imipramine |
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Yasmin
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combination oral contraceptive
ethinyl estradiol plus drospirenone drospirenone is a combination which has pregestin and anti-aldosterone effects which causes LESS flud retention blocks receptors for aldosterone |
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Progestin-Only Oral Contraceptives
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referred to as "mini pills"
ADEs: less effective cause more menstrual irregularities Benefits: do not cause thromboembolic disorders do not cause breast CA |
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Combination contraceptives with novel delivery systems
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transdermal contraceptive patch
vaginal contraceptive ring |
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transdermal contraceptive patch
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not for obese/overweight patients
preferred site of application is the abdomen |
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long-acting contraceptives
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subdermal levonorgestrel implants
depot medroxyprogesterone acetate (MPA) intrauterine devices spermicides barrier devices: condoms (male or female) diaphragm cervical cap |
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subdermal levonorgestrel implants
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long acting contraceptive
most effective |
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subdermal levonorgestrel
implants ADEs |
high incidence of side effects
(acts as progestin only oral contraceptives) menstrual irregularities breast discharge cervicitis musculoskeletal pain abdomnal discomfort leukorrhea vaginitis |
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Depot medroxyprogesterone acetate (MPA)
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depot madroxyproggesterone acetate PLUS estradiol cypionate (lunelle)
(IM injections every 28-30 days) |
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Depo Prova
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IM or SC injection for 3 month protection (does not contain estrogen)
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Depot medroxyprogesterone acetate (MPA)
effects and approval |
supresses ovulation
thickens cervical mucous alters endometrium approved in 1992 prolonged side effects cancer in lab animals concern of bone loss (osteoporosis) |
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long acting contraceptives
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intrauterine devices
spermicides barrier devices |
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intrauterine devices
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long-acting contraceptive
highly reliable not for patients with risk for STD multiple sexual partners |
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spermicides
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dispensed in:
foam gels vaginal films sponge creams suppositories no prescription needed minimal side effects moderately effective |
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spermicides
hiv and STDs |
spermacides containing nonoxylnol-9
have been linked to increase transmission of HIV NO STD protection |
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barrier devices
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condoms - male and female
protect against STDs |
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Diaphragm
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must be fitted and use spermicide
leave in no longer than 24 hours (toxic shock) 18% failure |
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cervical cap
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must be fitted and use spermicide
must remain in 8 hours after intercourse but no longer than 24 hours high failure rate |
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Drugs for medical abortion
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Mifepristone (RU 486) with misoprostol
methotrexate with misoprostol prostaglandins: misoprostol (PO) carboprost (IM) dinoprostone (vaginal inserts, vaginal suppostiories, gels) |
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Mifepristone (RU 486) with misoprostol
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blocks uterine progesterone receptors
99% effective for termination of early pregnancy **must be used within 7 days of conception ** |
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Infertility
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a decreased ability to reproduce
when medical treatment is implemented, 1/2 of infertile couples achieve pregnancy |
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sterility
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complete absence of reproductive ability
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causes of female infertility
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anovulation and
failure of follicular maturation unfavorable cervical mucous hyperprolactinemia endometriosis and scarring polycystic ovary syndrome (PCOS) |
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Anovulation
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without hormonal stimulation, ovulation will not occur (can be treated with drugs)
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unfavorable cervical mucous
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mucous too thick for sperm to travel
estrogen helps increase volume and consistency of unfavorable mucous |
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hyperprolactinemia
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can be caused by pituitary adenoma
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polycystic ovary syndrome (PCOS)
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may be helped with Metformin (insulin sensitizing drug)
help lose wight to help treat |
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causes of male infertility
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***most often due to number and motility of sperm or semen abnormality ***
hypogonadotroic hypogonadism erectile dysfunction idiopathic male infertility |
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hypogonadotropic hypogondism
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incapable of spermatogensis
treat with HCG human chorionic gonadotropin |
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Idiopathic male infertility
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no apparent cause
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Drugs to treat female infertility
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Clomiphene
clmid, milophene, serophene hhuman chorionic gonadotropin (hCG) menotropins [pergonal, repronex, menopur] Follitropins Lutropin alfa [liveris] choriogonadotropin alfa gonadotropin |
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Clompiphene
[clomid, milophene, serophene] Indications |
used to promote follicular maturation and ovulation
for amenorrhea take 1 pill a day for 5 consecutive days |
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Clompiphene
[clomid, milophene, serophene] MOA |
blocks receptors for estrogen
so pituitary secretes LH and FSH to stimulate ovulation and follicle maturation |
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Clompiphene
[clomid, milophene, serophene] ADEs |
hot flashes
GI: nausea, bloating abdominal discomfort breast engorgement visual disturbances: blurred vision multiple births ovarian hyperstimulation (very rarely) avoid during pregnancy |
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human chorionic gonadotropin (hCG)
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a polypeptide hormone produced by the placenta (acts like LH)
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human chorionic gonadotropin (hCG)
Indications |
promote follicular maturation and ovulation
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human chorionic gonadotropin (hCG)
ADEs |
ovarian hyperstimulation syndrome
edema injection site pain CNS disturbances: headache irritability restlessness fatigue |
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menotropins (pergonal, repronex, menopur)
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used in conjuction with hCG to promote follicular maturation and ovulation in anovulatory patients
have equal amounts of LH and FSH |
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menotropins (pergonal, repronex, menopur)
administration |
pergonal and repronex (IM)
menopu (SC) |
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menotropins (pergonal, repronex, menopur)
ADEs |
ovarian hyperstimulation syndrome
spontaneous abortions multiple births |
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Follitropins
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urofollitropin
follitropin alfa follitropin beta in women: acts directly on ovary to stimulate follicle stimulations in men: promoting spermatogenesis |
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Lutropin alfa [luveris]
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promote follicle maturation in infertile women with profound LH deficiency
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choriogonadotrophin alpha
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induces ovulation
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gonadotropin-releasing hormone antagonists
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used to prevent premature surge of endogenous LH in women who are undergoing controlled ovarian stimulation
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Cabergoline [Dostinex]
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better tolerated and more convenient than bromocriptine
used to correct amenorrhea and infertility assoc with excessive prolactin secretions activates dopamine receptors and inhibits prolactin secretion |
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Cabergoline [Dostinex]
ADEs |
nausea
headaches dizziness orthostatic hypotension |
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Leuprolide [lupron depot]
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suppresses ovarian hormone production which in turn suppresses endometriosis
for: endometriosis uterine fibroids central precocious puberty advanced prostate cancer |
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Leuprolide [lupron depot]
dosage and ADEs |
give IM monthly for 3 months
hot flashes vaginal dryness nasal irritation decreased libido bone loss mood changes headache |
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Danazol [danocrine]
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used to improve symptoms of endometriosis, but does not increase fertility
induce regression of endometrial implants |
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Danazol [danocrine]
ADEs |
acne
deepening of the voice growth of facial hair edema thrombotic events DVT educate them to go to the ER if developing dark, swollen and painful legs hepatotoxicity intensify effect of warfarin |
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Endometriosis - Educate
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Surgery reduces symptoms and can enhance fertility
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Oxytocics
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drugs that stimulate uterine contraction
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Tocolytics
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drugs that suppress contraction
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Oxytocics -
3 applications |
1) induction or augmentation of labor
2) control of postpartum bleeding 3) induction of abortion |
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Tocolytics - Indications
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supression of preterm labor
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drugs that promote cervical ripening...
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are used to soften the cervix before induction of labor
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uterine relaxants (tocolytics)
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magnesium sulfate
beta2 selective adrenergic agonists ritodrine terbbutaline [brethine] nifedipine [procardia, adalat, nifedical] indomethacin [indocin] |
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magnesium sulfate IV
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treatment of choice for suppressing preterm labor
inhibits acetylcholine release at uterine neuromuscular function preffered drug of choice for prevention of treatment of seizures assoc with eclampsia and severe pre-eclampsia **** requires frequent assessment of respirations **** |
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Beta 2 selective adrenergic agonist
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Ritodrine
terbutaline [bethine] |
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Ritodrine
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affects all beta cells
relaxes uterus smooth muscles thereby decreasing freq and intensity as effective as magnesium sulfate but with much greater risk to the mother |
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Ritodrine ADEs
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pulmonary edema
hypotension hyperglycemia tachycardia in mother tachycardia in fetus |
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Terbuttaline [Brethine]
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indicated for asthma but used to delay preterm labor
(not fda approved) |
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Nifedipine
(procardia, adalat, nifedical) |
calcium channel blockers to suppress preterm labor
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indomethacin (indocin)
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second-line drug for suppressing preturn labor
reserved for women who are unresponsive or intolerant of preferred agents |
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Oxytocic Drugs
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stimulate uterine contraction
induction or augmentation of labor control of postpartum bleeding induction of abortion |
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Tocolytic Drugs
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suppresses contractions
suppression of preterm labor |
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Oxytocin [pitocin]
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peptide hormone produced by the posterior pituitary to induce labor by promoting uterine contraction
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oxytocin [pitocin]
physiologic and pharmalcologic effects |
uterine stimulation
increased force freq and duration of contractions milk ejection water retention (similar to ADH) |
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Oxytocin [pitocin]
precautions and contraindications |
uterine rupture may occur
**** discontinue in presnce of contractions lasting > 60 sec **** women with active genital herpes |
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Oxytocin [pitocin]
ADEs |
water intoxication d/t antidiuretic affects
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Oxytocics - indications
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(uterine stimulants)
pregnancy beyond term early vaginal delivery to reduce morbidity and mortality of mother and infant (premature rupture of veins) |
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oxytocics - precautions and contraindications
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Caution if fetal lungs are not mature or if cervis is not ripe
contraindications: can cause utterine rupture |
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Ergot Alkaloids
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ergovine
methylergonovine dried preparation of Claviceps purpurea (fungus on rye plant) |
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Ergot Alkaloids - Indications
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post partum use (bleeding)
aumentation of labor (not recommended) dose dependent for contractions but not for induction of labor migraine (constricts cerebral blood vessels) usually reserved for hemorrhagic emergencies |
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ergot alkaloids - ADEs
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IV admin: hypertension d/t constriction of arterioles and veins
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ergonovine
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used in the presence of a boggy uterus and vaginal bleeding
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Carboprost tromethamine (hemabate)
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uterine stimulant
preferred agen for controlling postpartum hemorrhage causes intense uterine contractions |
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carboprost tromethamine [hemabate]
ADEs |
GI reactions
vomiting and diarrhea fever vasoconstriction constricion of the bronchi |
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Dinoprostone [prepidil, cervidil]
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used for promoting cervial ripening before induction of labor with oxytocin
gel, vaginal inserts |
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misoprostol [cytotec]
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**** not approved for cervical ripening ****
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peptic ulcer disease (PUD)
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a group of upper GI disorders characterized by varying degrees of erosion of the gut wall
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Peptic ulcers
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develop with there is an imbalance b/t mucosal defensiv factors and aggressive factors
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Ulceration
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most common in the lessure curvature of the stomach and duodenum, although they may develop in any region exposed to acid and pepsin
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H. pylori
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most cases of PUD are caused by infection with H. pylori
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Peptic Ulcers
defensive factors |
mucous
bicarbonate blood flow prostaglandins |
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Peptic ulcers -
aggressive factors |
H. pylori
NSAIDs Gastric Acid Pepsin Smoking |
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Peptic Ulcers
Mucus |
secreted by cells of the GI mucosa to form a barrier
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Paptic Ulcer and Bicarbonate
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secreted by epithelial cells of the stomach and the duodenum and from pancreas bicarbonate is secreted into the duodenum
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Peptic Ulcer and blood flow
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essential for mucosal integrity
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Pepit Ulcer and Prostaglandins
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stimulate secretion of mucous and bicarbonate and promote vasodilation and suppression of gastric acid
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Drugs for peptic Ulcer Dises
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Paptic ulcer disease:
upper GI disorders degrees of erosion of the gut wall Cause: imbalance b/t mucosal and aggressive factors |
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h.pylori and peptic ulcers
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ingested
unaffected by acid colonizes and remains for decades (most common cause of gastric and duodenal ulcers) |
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NSAIDS and ulcers
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drug induced cause of gastric and duodenal ulcers
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Gastric Acids and ulcers
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acid injures mucosal cells and activated pepsin
Zollinger-Ellison syndrome: hypersecretion of acid to form ulcer |
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Pepsin and Ulcers
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proteolytic enzyme present in gastric juice and can injur unprotected cells
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Smoking and Ulcers
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delays ulcer healing and increases risk of recurrence
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Goal of Ulcer Drug Therapy
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alleviate symptoms
promote healing prevent complications preven recurrence |
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casses of antiulcer drugs
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antibiotics
(only antibiotics alter disease process) antisecretory agents mucosal protectants antisecretory agents that enhance mucosal defenses antacids |
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H. pylori test
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breat test or serum
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H. pylori treatment
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two antibiotics are prescribed
-Bismuth compounds (pepto-bismol, tritec w/added ranitidine) topically to disrupt cell wall of H. pylori, inhbit urease activity preventing h.pylori adhereing to gastric surface * may color tongue or blacken stool |
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H. pylori
clarithromycin |
inhibits protein synthesis
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H. pylori
amoxicillin |
disrupts cell wall
common side effect: diarrhea |
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H. pylori
tetracycline |
inhibits protein synthesis
stains teeth avoid in pregnancy |
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H. pylori
metronidazole |
avoid pregnancy and ETOH
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NSAID- Induced Ulcers
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prophylaxis (misoprostol is approved for prophylaxis of NSAID-induced ulcers
omeprazole may be just as effective and better tolerated |
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NSAID-Induced Ulcers
Evaluation |
monitor for relief of pai and preform radiologic or endoscopic examination of ulcer site; test for eradication of H.pylori
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Histamine 2 receoptor antagonists
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first choice for ulcers
cimetidine ranitidine ranitidine bismuth citrate famotidine nizatidine |
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cimetidine [tagament]
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H2 cells are located in the parietal cells of the stomach
blocks H2 receptor - reduces volume and acid concentration suppresses basal acid secretion and reduces stimulation of acid secretion by gastrin and acetylcholine |
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cimetidine [tagament]
dosing, pharm |
PO, IV, IM
food decreases absorption crosses BBB Metabolized in liver Excreted in Urine |
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cimetidine [tagamet]
ADEs |
gynecomastia
reduced libido impotence elderly (renal/hepati impairment, CNS depression/excitation, confusion) |
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Cimetidine [tagamet]
Interactions |
increases warfarin, dilantin, theophylline
anacids decrease effect (give one hour apart) |
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Ranitidine [Zantac]
|
more potent, fewer side effects than, and less interactions than with cimetidine
blocks H2 receptors on parietal cells PO, IM, IV food no effect on absorption, eleminated hepatic and renal adverse effects are rare |
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Ranitidine bismuth citrate [Tritec]
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pepto-bismol plus ranitidine
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Famotidine[pepcid]
|
similar to ranitidine
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Nizatidine [axid]
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similar to ranitidine
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Proton pump inhibitors
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omeprazole (prilosec)
esomeprazole (nexium) lansoprazole (prevacid) rabeprazole (aciphex) pantoprazole (protonix) |
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Omeprazole
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prilosec
powerful suppressant of gastric secretion irreversibly inhibits the enzmes needed to produce stomach acid inhibits H+, basal acids release |
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Omeprazole - pharm
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short half life
(reduces acid production 97% in 2 hours) used for short-term therapy (long term caused cancer in rats) |
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Omeprazole - ADEs
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headache
GI |
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Omeprazole - Pharmacokinetics
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administered PO
capsule dissolves in stomach, granules dissolve duodenum metabolized in liver excreted in urine |
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Omeprazole - Interactions
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reduces absorption of atazanavir (anti-viral)
ketoconazole (Nizoral) itraconazole (sporonox) |
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esomeprazole
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nexium
nearly identical to prilosec metabolized slower making effects last longer |
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Lansoprazole
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prevacid
similar to prilosec take dose before breakfast |
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Rabeprazole
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aciphex
similar to prilosec and prevacid |
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Pantoprazole
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protonix
does not effect the metabolism of other drugs |
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Sucralfate [carafate]
|
protective barrier up to 6 hours
forms a sticky gel that adheres to ulcer and creates a protective barrier against pepsin and acid eliminated in stool take 1 hour before meals |
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Sucralfate [carafat] ADEs and INteractions
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ADE: constipation
Interactions: antacids interfere with effectiveness (take 30 min apart) |
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Misoprostol [cytotec]
|
analog of prostaglandin E1
prostaglandins protect by suppressing gastric acids, promote secretion of bicarbonate and mucous and maintaining blood flow only for prevention of gastric ulcers caused by long term NSAIDs |
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nisoprostol [cytotgec]
ADES and warnings |
ADE: diarrhea, dysmennorhea
*** not for pregnancy or use with caution during child bearing years (must use with birth control)*** |
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Antacids
|
alkaline compounds to neutralize stomach acid;
used in peptic ulcer disease and gastroesphageal reflux disase |
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Antacids
beneficial actions |
neutralizing acid decreases destruction of gut wall
if pH greater than 5, get decrease in pepsin may enhance mucosal protection by stimulating production of prostaglandins poorly absorbed except for sodium bicarbonate |
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antacids
Indications |
peptic ulcer disease
admined before anestheiia to prevent aspirtion pneumonitis used prophylactically to prevent stress ulcers |
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Antacids
ADEs |
constipation (aluminum hydroxide)
diarrhea (mg hyroxide) some contain substantial amounts of sodium, which can exacerbate HTN and HF |
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Antacids
Interactions |
by increasing pH, can affect dissolution and absorption;
can change urinary pH |
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Four groups of Antacids
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aluminum compounds
magnesium compounds calcium compounds sodium compounds |
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magnesium hydroxide
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rapid-acting
long duration of action common problem is diarrhea avoid in pts with potential intestinal problems used as a laxative |
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aluminum hydroxide
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slow acting
long duration significant amts of Na in agents get constipation absorbes compounds tetracycline, warfarin, digoxin can cause hypophospatemia |
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calcium carbonate
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rapid acting
long duration get acid rebound get constipation can cause eructation and flatulence |
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sodium bicarbonate
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unfit for treating ulcers
rapid onset but short acting increases intraabdominal pressure absorption of sodium exacerbates HTN and HF if renal impairment, get systemic alkalosis |
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peptic ulcers -- treatment
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eat smaller more frequent meals
antacids containing sodium should be taken with caution in pt with heart or blood pressure problems spicy foods DO NOT add or create peptic ulcers! |
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Laxatives
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used to ease or stimulate defecation
these agents can soften the stool increase stool volume hasten fecal passage through intestine facilitate evacuation from the rectum |
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Function of the colon
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absorb water and electrolytes
absorbes 50% of the 1500mL water that enters colon minimal absorption of nutrients proper function is dependent on dietary fiber (needs 30-60 g/day) absorb water to soften stool and bulk up stool digested by colonic bacteria to increase fecal mass |
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constipation
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determined by degree of harness of stool
caused by deficiency of fiber and fluids excercise helps may be drug induced |
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Laxatives - Indications
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used to ease or stimulate defecation
soften the stool helps with discomfort and reduces straining in heart pts and pts with hemorrhoids hasten fecal passage though the intestine before procedure or surgery failitate evacuation from the rectum |
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laxatives - containications
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abdominal pain
nausea cramps other symptoms of appendicitis regional enteritis diverticulitis ulcerative colitis acute surgical abdomen |
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Laxative Categories
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accounding to mechanism of action
bulk forming laxatives surfactants stimulants osmotics |
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Laxative Classification by time
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Group 1 (act in 2-6 hrs)
group 2 (act in 6-12 hrs) group 3 (act in 1-3 days) |
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bulk forming laxatives
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fuction like dietary fiber
category III Psyllium (metamucil) can obstruct esophagus give with 240mL water to avoid impaction |
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surfactant laxatives
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inhibits h2O absorption
Cat III Docusate sodium (colace) |
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Stimulant laxatives
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increase motility and inhibit h2O
oral is cat II suppository cat I bisacodyl [dulcolax] swallow pill intact |
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osmotic laxatives
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salts that hold h20 in bowel
increases mass and stretches wall to promote peristalsis low dose cat II high dose cat I Milk of Magnesia Magnesium hydroxide and sodium phosphate |
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Laxative Abuse
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Misconception: good health consists of a daily and bountiful BM
causes diminished defecatory reflex leads to reliance on laxatives electroyle imbalance, dehydration and colitis |
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Laxative - Education
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do not use laxatives if experiencing ab cramps n/v
it taking mg hydroxide laxative, the pt needs to increase fluid intake laxatives with magnesium salts are contraindicated in renal or heart pts |
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antiemetics
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used to suppress vomiting
most important application is suppression of chemotherapy induced emesis |
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the emetic response
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complex reflex started by
activation of vomiting center either directly or indirectly indirect acting stimulates the chemoreceptor trigger zone (CTZ) |
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Receptors important in vomiting response
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serotonin, dopamine, acetylecholine, histamine
antiemetic drugs can block more than one receptor type |
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Antiemetics - Meds
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Ondansetron
Granisetron Dolasetron Palonosetron methylprednisolone dexamethasone |
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ondansetron [zofran]
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serotonin receptor antagonist
blocks type 5HT3 receptors in the brain serotonin rreceptors on afferent vagal neurons in upper GI more effective when used with dexamethasone |
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ondansetron [zofran]
ADEs and route |
HA, diarrhea, dizziness
PO or IV |
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Granisetron [Kytril}
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serotonin receptor antagonist
antiemetic ADEs: HA, weakness/tiredness diarrhea/constipation |
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Dolasetron [Anzemet}
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serontonin receptor antagonists
for prevention of chemo induced nausea |
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Palonosetron [Aloxil}
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serotonin receptor antagonist
antiemetic only IV use Longer half-life |
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Glucocorticoids as antiemetics
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more effective when used with other antiemetics
methylprednisolone dexamethasone |
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Antiemetics - dopamine antagonists
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phenothiazines
butyrophenones metoclopramide dronabinol |
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phenothiazines
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antiemetic
dopamine antagonist can cause anticholinergic effects, sedation and hypotension |
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butyrophenones
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haloperidol
droperidol antiemetic dopamine anagonist post-op nausea similar effects as phenothazines |
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metoclopramide
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Reglan
antiemetic dopamine antagonist |
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dronabinol
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Cannabinoid
antemetic dopamine antagonist principle psychoactive agent in MJ watch for the development of psyhchiatric disorders, hallucinations |
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Use of Antiemetics
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because there are different pathways to nausea use in combo therapy/meds to cover different pathways
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drugs for motion sickness
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scopolamin (muscarinic antagonist)
antihisamines |
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scopolamine
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muscarinic anagonist
for motion sickness supresses nerve traffic in neuronal pathway from inner ear to vomiting center |
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scopolamine
ADEs |
dry mouth
blurred vision drowsiness severe side effects - urinary retention constipation disorientation |
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Antihistamines for motion sickness
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dimenhydrinate (dramamine)
meclizine (andtivert) cyclizine (Marezine) |
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antidiarrheal agents
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opioids - diphenoxylate [lomotil]
loperamide [immodium] difenoxin paregoric opium tincture |
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diarrhea causes
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can be caused by infection, maldigestion, inflammation, and functional disorders of the bowel
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diphenoxlate [lomotil]
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activate opioid receptors in the GI tract
decrase intestinal motility slow intestinal transit more time for fluids and electrolytles to be absorbed |
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loperamide [immodium]
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comes OTC in tablet, capsule and liquid
antidiarrheal |
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difenoxin
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antidiarrheal
like diphenoxylate, give only with atropine |
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paregoric
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diluted solution of opium and contains morphine
antidiarrheal |
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opium tincture
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alcohol based solution with 10% opium by weight
high potential for abuse antidiarrheal |
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management of infectious diarrhea
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increases the time for bacteria to get out
give Azithromycin for infection (may be used in pregnancy) |
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Drugs for Inflammatory Bowel Disease (IBD)
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tricyclic antidepressants
Alosetrol [lotronex] tegaserod [zelnorm] aminosalicyclates Immunomodulators |
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Tricyclic antidepressants for IBD
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these drugs decrease ab cramping and pain
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Alosetron [Lotronex]
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potentially dangerous
for IBD for diarrhea prominent in IBS in women no known adverse effects with other drugs most common side effect is constipation approved for ulcerative colitis, diverticulitis, and intestional obstruction |
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Tegaserod [Zelnorm]
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approved for short term use in constipation prominent women with IBS and approved for renal impaired pts
most common ADE: diarrhea |
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Aminosalicylates
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sultasalazine [Azulfidine]
similar to sulfonamide reduced inflammation mesalamine dissolve in terminal ileus and suppository Osalazine [dipentum] ADE: watery diarrhea |
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Glucocortocoids for IBD
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dexamthasone and budesonide
(anti-inflammatory) |
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immunomodulators
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azathioprine and mercaptopurine
for non responders cyclosporine cause renal dysfunction neurotoxicity and suppress immune infliximab [Remicade] |
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metoclopramide
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suppresses emesis and
increases GI motility used for suppressing nausea in chemotherapy decreases chemoreceptor stimulation ADEs: sedation and diarrhea |
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Palifermin [Kepviance]
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first drug for decreasing oral mucositis
stimulates proliferation, differentiation and migration of epithelial cells only for pts with hematologic malignancies most commmon reactions involve skin and mouth binds with heparin |
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pancreative enzymes
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Lipase
amylase chyrmotrypsin Trypsin helps with digestion of fats may need antacids and histamine (H2 blockers) to be used with pancreatice enzymes take with all meals and snacks |
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Drugs to dissolve gall stones
cholelithiasis |
chenodeoxycholic acid [chenodiol]
ursodeoxycholic Acid [ursodiol] |
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chenodeoxycholic acid [chenodiol]
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for cholelithiasis to dissolve gallstones
reduces hepatic production of cholesterol which dissolves radiolucent stones (not for radiopaque stones) |
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Ursodeoxycholic Acid [Ursodiol]
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reduced cholesterol conent of bile
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