Adrenal Agents. Women's Health Agents. Men's Health Agents

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GLUCOCORTICOIDS
AND
MINERALOCORTICOIDS
Corticosteroids
 Adrenal glands produce glucocorticoids and
mineralocorticoids
 Glucocorticoids:

Involved in cholesterol, fat, and protein
metabolism
Corticosteroids
 Adrenal glands produce glucocorticoids and
mineralocorticoids
 Glucocorticoids:

Involved in cholesterol, fat, and protein
metabolism
 Mineralocorticoids:

Involved in regulating electrolyte and water
balance
Cortisol
 Principal adrenal steroid hormone
 Responsible for:
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Gluconeogenesis
Protein catabolism
Anti-inflammatory reactions
Stimulation of fat deposition
Sodium and water retention
Corticosteroids
 Adrenal hormones excluding sex hormones
 Steroid production follows a circadian rhythm
Properties of glucocorticosteroides
used in clinics
 Anti-inflammatory
 Immune-depressive
 Anti-allergic
 Anti-shock
 Anti-toxic
Anti-inflammatory action of
GCS
 Nonspecific inflammation
 Auto-immune component
 Hyperergic character
 Therapy of despair
Mechanism of anti-inflammatory action of GCS
GCS
activation of lipomoduline
decreasing of activity of phospholipase А2
slowing down of arachidonic acid
metabolites production
(prostaglandins, leucotriens,
thromboxan А2)
stabilization
of cellular and
lyzosomal
membranes
depression of
histamine, serotonin,
bradykinine releasing
decreasing of
leucocytes’
migration processes,
depression of
phagocytes activity
decreasing of capillaries’
wall permeability
Indications for administration of
GCS
 Insufficiency of adrenal cortex
 Rheumatoid illnesses (rheumatoid arthritis, rheumatism, system
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red lupus etc.)
Chronic active hepatitis
Bronchial asthma
Ulcerative colitis
Nephritic syndrome
Auto-immune hemolytic anemia
Shock and collapse of any etiology
Brain, lungs, larynx edema
Acute allergic reactions
Transfusion reactions
Heavy infections (hiding behind the etiotropic drugs!)
Liver disesaes
Doses and terms of GCS therapy
Situation
Acute cases (shock, collapse,
brain, lungs edema, septic
shock, asthmatic condition
etc.)
Daily dose
200-500800-1000 mg
i.v.
Terms of
treatment
1-3 days
Subacute and acute attacks of 20-50 mg
4-6 weekschronic processes
(rarely till 200 several
(rheumatoid diseases,
mg)
months
ulcerative colitis, bronchial
asthma etc.)
Primary and secondary
2,5-10 mg
insufficiency of adrenal cortex
life-long
Corticosteroids
 Act as anti-inflammatory and
immunosuppressive agents in treating
diseases of different origins:
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Hematologic
Allergic
Inflammatory
Neoplastic
Autoimmune
Addison’s Disease
 Life-threatening deficiency of glucocorticoids
and mineralocorticoids
 Treated with daily corticosteroids
Symptoms of Addison’s Disease
 Debilitating weakness
 Hyperkalemia
 Hyperpigmentation of skin
 Low levels of serum sodium and glucose
 Reduced blood pressure
 Weight loss
Cushing’s Disease
 Caused by an overproduction of steroids or
excessive administration of corticosteroids
 Symptoms:

Protruding abdomen; round, puffy face; fat
over the shoulder blades
Reasons for Using Corticosteroids
 Inhibit inflammation
 Useful in treating asthma, rashes, and skin
disorders
 Available in many different dosage forms
Problems with Corticosteroids
 Lessen the ability of leukocytes to destroy
infection which decreases fever, redness, and
swelling
 Also may cause infection to spread
Corticosteroid Dispensing Issues
Warning!
 Take caution in patients with diabetes,
uncontrolled hypertension, CHF, severe
infection or altered immunity, or peptic ulcer
disease with active GI bleeding
Corticosteroids
 Usage must be tapered off, not abruptly
stopped
 May cause withdrawal symptoms

Anorexia, nausea, vomiting, myalgia,
arthralgia, lethargy, headache, sluggishness,
weight loss, postural hypotension, fever and
depression
 Doses should be given in the morning
Adverse Effects of Glucocorticoids
 Cardiovascular effects
 Dermatologic effects
 Gastrointestinal effects
 Immune system effects
 Metabolic effects
 Musculoskeletal effects
 Neuropsychiatric effects
 Ophthalmic effects
Adrenal Sex Hormones
 Androgens are produced by:
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The testes
The ovaries
Adrenals
Peripheral fat tissue
 Most important male hormone is testosterone
which is produced by the testes
Responsibilities of Testosterone
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Initiating sperm production
Behavioral characteristics
Libido
Sexual potency
Muscle mass and strength
Fat distribution
Bone mass
Erythropoiesis
Prevention of baldness
Hypogonadism
 Deficient hormone production and secretion
 Androgens must be replaced by medications
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May cause virilization, muscle building, and
hematologic stimulation of erythropoiesis
Can be used to treat anemia, breast cancer, or
endometriosis
Androgen’s Side Effects
 Virilization
 Hirsutism
 Acne
 Hepatoxicity
 High levels of erythrocytes
 Oily skin
 Gynecomastia
 Priapism
Male Impotence
 Failure to initiate or maintain an erection until
ejaculation
 Causes:
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Testosterone deficiency
Alcoholism
Cigarette smoking
Psychological factors
Medications
Drugs That May Cause Impotence
 Alcohol (most
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significant)
Amphetamines
Antihypertensives
Corticosteroids
Estrogens
 H2 blockers
 haloperidol
 lithium
 Opiates
 Some antidepressants
Drug List
Agents for Male Impotence
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alprostadil (Caverject, Edex, Muse)
danazol (Danocrine)
methyltestosterone (Android, Testred)
oxymetholone (Anadrol)
papaverine
testosterone (Androderm, AndroGel, Striant,
Testoderm)
Drug List
Agents for Male Impotence
– Phosphodiesterase Inhibitors
 sildenafil (Viagra)
 tadalafil (Cialis)
 vardenafil (Levitra)
sildenafil (Viagra)
 1st oral therapy for impotence
 Allows an erection to occur naturally
 Take at least 1 hour before activity
sildenafil Dispensing Issues
Warning!
 Potentially lethal interaction with nitrates
tadalafil (Cialis)
 Duration of action is 36 hours
 Faster onset and longer duration than others
in this class
tadalafil Dispensing Issues
Warning!
 Potentially lethal interaction with nitrates
Female Hormones
 Can prevent conception, ease symptoms of
menopause, and help prevent osteoporosis
 2 main female hormones:
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Estrogen
Progesterone
Estrogen
 Formed in the ovaries when FSH is released
 Responsible for:
 Endometrial growth
 Increased cervical mucus
 Cornification of vaginal mucosa
 Growth of breast tissue
 Increased epiphyseal closure
 Sodium retention
 Carbohydrate metabolism
 Calcium utilization
Estrogen Deficiency Symptoms
 Irregular bleeding and cycles
 “hot flashes” that start in the face and move
down through the body
 Atrophic vulvovaginitis, excessive dryness
 Dyspareunia
 Frequent infections
Menopause
 As women reach menopause estrogen
production decreases
 HRT can be used to supplement estrogen
levels
estrogens Dispensing Issues
Warning!
 Patients should not smoke during therapy,
whether birth control or HRT
Estrogen’s Side Effects
 Nausea
 Vomiting
 Bloating
 Weight gain
 Breast tenderness
 Breakthrough bleeding
 Glucose intolerance
HRT
 Reduces symptoms of menopause
 Decreases bone loss
 Lowers risk of cardiovascular disease
 Small risk of breast cancer
Drug List
Estrogens
 conjugated estrogen (Enjuvia,Premarin)
 conjugated estrogen-medroxyprogesterone
(Premphase, Prempro)
 estradiol (Alora, Climara, Esclim, Estrace,
Estraderm, Estrasorb, Estring, Femring,
Menostar, Vivelle, Vivelle Dot)
Drug List
Estrogens
 estradiol-levonorgestrel (Climara Pro)
 estradiol-norethindrone (Activella,
CombiPatch)
 estradiol-norgestimate (Ortho-Prefest)
Drug List
Estrogens
 estropipate (Ogen)
 ethinyl estradiol (Estinyl)
 ethinyl estradiol-norethindrone (Femhrt)
estrogen-medroxyprogesterone
(Premphase, Prempro)
 Provides estrogen and progesterone
replacement
 Prevents uterine cancer
Progestins
 Used primarily in birth control and to prevent
uterine cancer
 Also used for menstrual dysfunction
Progestin’s Side Effects
Similar to pregnancy:
 Weight gain
 Depression
 Fatigue
 Acne
 Hirsutism
Drug List
Progestins
 levonorgestrel (Norplant II)
 medroxyprogesterone (Depo-Provera,
Provera)
 norethindrone (Micronor)
Contraceptives
 Most OCs are combinations of estrogen and
progestin
 Interfere with hormones responsible for
regulation of the menstrual cycle
 Change the consistency of cervical mucus
 Alter the endometrial lining
Benefits of OCs
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Prevention of pregnancy
Regulates menstrual cycle
Reduces menstrual flow
Lessens severe menstrual cramps and pain
Protects against ovarian and endometrial
cancer, benign breast disease, ectopic
pregnancy, fibroadenomas, and ovarian cysts
Oral Contraceptives
 There are different combinations of estrogen
and progestin as well as differing strengths
 Tricycling – taking meds for 3 - 21 day cycles
without a pill-free interval
Drug List
Contraceptive Agents
 estradiol cypionate-medroxyprogesterone
(Lunelle)
 ethinyl estradiol-desogestrel (Cyclessa,
Desogen, Kariva, Mircette, Ortho-Cept)
 ethinyl estradiol-drospirenone (Yasmin)
Drug List
Contraceptive Agents
 estradiol cypionate-medroxyprogesterone
(Lunelle)
 ethinyl estradiol-desogestrel (Cyclessa,
Desogen, Kariva, Mircette, Ortho-Cept)
 ethinyl estradiol-drospirenone (Yasmin)
Drug List
Contraceptive Agents
 ethinyl estradiol-ethynodiol diacetate
(Demulen)
 ethinyl estradiol-etonogestrel (NuvaRing)
 ethinyl estradiol-levonorgestrel (Levlen,
Nordette, Seasonale, Tri-Levlen, Triphasil,
Trivora-28)
Drug List
Contraceptive Agents
 ethinyl estradiol-norelgestromin (Ortho Evra)
 ethinyl estradiol-norethindrone (Estrostep Fe,
Femhrt, Loestrin Fe, Ovcon)
 ethinyl estradiol-norgestimate (Ortho TriCyclen, Ortho Tri-Cylcen Lo)
Drug List
Contraceptive Agents
 ethinyl estradiol-norgestrel (Lo/Ovral, Low-
Ogestrel, Ovral)
ethinyl estradiol-desogestrel (Cyclessa,
Desogen, Kariva, Mircette, OrthoCept)
 Inhibits ovulation
 Includes 2 days of placebo followed by 5
days of low-dose estrogen
 May be safer for smokers
ethinyl estradiol-levonorgestrel
(Seasonale)
 Taken for 3 months at a time
 Patient only has 4 menses per year
 Prevents egg release from the ovaries,
increases mucus thickness, and thickness of
the endometrial lining
ethinyl estradiol-dropirenone (Yasmin)
 Drospirenone is related to spironolactone (a
diuretic)
 Causes less bloating and less weight gain
 May cause weight loss due to excess water
loss
ethinyl estradiol-norelgestromin
(Ortho-Evra)
 Transdermal contraceptive
 Suppresses gonadotropins
 A new patch is applied every 7 days for
weeks then the 4th week is patch free
3
Some Oral Contraceptive Interactions
 Antibiotics
 Anticonvulsants
 Antifungals
 Benzodiazepines
 Bronchodilators
 Corticosteroids
 Lipid-lowering agents
 TCAs
Emergency Contraception
 In great demand
 Patients want them to be available OTC
Discussion
What is one of the arguments for
emergency contraceptives being OTC?
Discussion
What is one of the arguments for
emergency contraceptives being OTC?
Answer: After making a doctor’s
appointment and then going to the get
the prescription, sometimes it is too
late to take the medication
Drug List
Contraceptive Agents
Emergency Contraceptives
 levonorgestrel (Plan B)
 norgestrel (Ovrette)
Home Pregnancy Tests
 Critical organ systems develop in the first
month which is affected by
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Mother’s diet
Environment (smoking)
Medications
Consumption of alcoholic beverages
Home Pregnancy Tests
 Based on detecting human chorionic
gonadotropin (HCG)
 Levels can be measured as early as 6-8 days
after conception
 Results are given within 1-5 minutes
 Tests are better than 95% accurate
Drugs Used at Birth
 Often no drugs are necessary for delivery, but
in some cases they are
 To restart labor
 To decrease uncontrolled bleeding
Drug List
Drugs Used at Birth
 methylergonovine (Methergine)
 oxytocin (Pitocin)
oxytocin (Pitocin)
 Natural hormone that stimulates uterine
contractions
 Drug should be used as a last resort
oxytocin’s Side Effects
For the woman:
For the child:
 Vomiting
 Bradycardia
 Irregular heart rate
 Arrhythmias
 Tachycardia
 Jaundice
 Postpartum bleeding
Sexually Transmitted Disease
 the structural anatomy of the male and
female genital systems
Gonorrhea
 Most commonly reported STD
 Caused by Neisseria gonorrhoeae that
attaches to mucosal cells in:
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Oropharyngeal area
Eye
Joints
Rectum
Male and female genitalia
Gonorrhea
 If untreated, it can cause systemic infection
including
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The heart, meninges, eyes, pharynx, and
joints
 Eye infections occur most often in newborns
and can cause blindness
Syphilis
 Caused by Treponema pallidum
 Incubation averages three weeks
 Infection develops in 3 stages:
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Primary stage
Secondary stage
Tertiary stage
Primary-Stage Infection
 Small, hard-based sore develops at site of
infection
 May be painless and patient may be unaware
 Fluid in the sores is highly infectious
 Bacteria enters the bloodstream and
lymphatic system
Secondary-Stage Infection
 Produces skin rashes, patchy hair loss,
malaise, and mild fever
 Symptoms subside after a few weeks and
disease becomes latent
 After 2-4 years of latency, the disease is
usually no longer infectious
Tertiary-Stage Infection
 Occurs after an interval of at least 10 years
 Lesions appear as a rubbery mass in many
organs and sometimes the skin
 May cause extensive damage
Congenital Syphilis
 Crosses the placenta into the fetus
 Results in neurologic damage if pregnancy
occurs during the tertiary stage
 Pregnancy during primary or secondary stage
is likely to produce a stillborn child
Genital Herpes
 Caused by herpes simplex virus
 Lesions appear after 1 week of incubation
 Infectious vesicles appear and heal within 2
weeks
 Virus becomes latent until reactivated
Candidiasis
 Caused by Candida albicans
 Yeast-like fungal infection that can cause
infection in genital area of men and women
and the mouth (thrush)
 Can cause itching and a thick, yellow, cheesy
discharge
Vaginitis
 Caused by Gardnerella vaginitis
 Results from interaction between this
organism and anaerobic bacterium in the
vagina
 Symptoms: frothy discharge with fishy odor
and vaginal pH of 5 to 6
Vaginitis
 May also be caused by Trichomonas
vaginalis
 Normally found in both sexes, but causes
infection if vaginal pH changes
 Causes profuse yellowish or cream-colored
discharge with a disagreeable odor, irritation,
and itching
Drug List
Agents for STDs
 acyclovir (Zovirax)
 azithromycin (Zithromax)
 ceftriaxone (Rocephin)
 clotrimazole (GyneLotrimin, Mycelex)
 doxycycline (Doryx, Vibramycin)
Drug List
Agents for STDs
 erythromycin
 fluconazole (Diflucan)
 ketoconazole (Nizoral)
 metronidazole (Flagyl)
 miconazole (Monistat)
Drug List
Agents for STDs
 penicillin G benzathine (Bicillin L-A)
 spectinomycin (Trobicin)
 tetracycline (Sumycin)
 tioconazole (Vagistat-1)
 valacyclovir (Valtrex)
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