GLUCOCORTICOIDS AND MINERALOCORTICOIDS

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GLUCOCORTICOIDS AND MINERALOCORTICOIDS
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Corticosteroids

• Adrenal glands produce glucocorticoids and
  mineralocorticoids
• Glucocorticoids
• Involved in cholesterol, fat, and protein
  metabolism

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Corticosteroids

• Adrenal glands produce glucocorticoids and
  mineralocorticoids
• Glucocorticoids
• Involved in cholesterol, fat, and protein
  metabolism
• Mineralocorticoids
• Involved in regulating electrolyte and water
  balance

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Cortisol

• Principal adrenal steroid hormone
• Responsible for
• Gluconeogenesis
• Protein catabolism
• Anti-inflammatory reactions
• Stimulation of fat deposition
• Sodium and water retention

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Corticosteroids

• Adrenal hormones excluding sex hormones
• Steroid production follows a circadian rhythm

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Properties of glucocorticosteroides used in
clinics

• Anti-inflammatory
• Immune-depressive
• Anti-allergic
• Anti-shock
• Anti-toxic

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Anti-inflammatory action of GCS

• Nonspecific inflammation
• Auto-immune component
• Hyperergic character
• Therapy of despair

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Mechanism of anti-inflammatory action of GCS
GCS
activation of lipomoduline
decreasing of activity of phospholipase ?2
slowing down of arachidonic acid metabolites
production (prostaglandins, leucotriens,
thromboxan ?2)
stabilization of cellular and lyzosomal membranes
decreasing of capillaries wall permeability
decreasing of leucocytes migration processes,
depression of phagocytes activity
depression of histamine, serotonin,
bradykinine releasing
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Indications for administration of GCS

• Insufficiency of adrenal cortex
• Rheumatoid illnesses (rheumatoid arthritis,
  rheumatism, system 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

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Doses and terms of GCS therapy
Situation Daily dose Terms of treatment
Acute cases (shock, collapse, brain, lungs edema, septic shock, asthmatic condition etc.) 200-500- 800-1000 mg i.v. 1-3 days
Subacute and acute attacks of chronic processes (rheumatoid diseases, ulcerative colitis, bronchial asthma etc.) 20-50 mg (rarely till 200 mg) 4-6 weeks- several months
Primary and secondary insufficiency of adrenal cortex 2,5-10 mg life-long
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Corticosteroids

• Act as anti-inflammatory and immunosuppressive
  agents in treating diseases of different origins
• Hematologic
• Allergic
• Inflammatory
• Neoplastic
• Autoimmune

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Addisons Disease

• Life-threatening deficiency of glucocorticoids
  and mineralocorticoids
• Treated with daily corticosteroids

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Symptoms of Addisons Disease

• Debilitating weakness
• Hyperkalemia
• Hyperpigmentation of skin
• Low levels of serum sodium and glucose
• Reduced blood pressure
• Weight loss

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Cushings Disease

• Caused by an overproduction of steroids or
  excessive administration of corticosteroids
• Symptoms
• Protruding abdomen round, puffy face fat over
  the shoulder blades

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Reasons for Using Corticosteroids

• Inhibit inflammation
• Useful in treating asthma, rashes, and skin
  disorders
• Available in many different dosage forms

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Problems with Corticosteroids

• Lessen the ability of leukocytes to destroy
  infection which decreases fever, redness, and
  swelling
• Also may cause infection to spread

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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

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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

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Adverse Effects of Glucocorticoids

• Cardiovascular effects
• Dermatologic effects
• Gastrointestinal effects
• Immune system effects
• Metabolic effects
• Musculoskeletal effects
• Neuropsychiatric effects
• Ophthalmic effects

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Adrenal Sex Hormones

• Androgens are produced by
• The testes
• The ovaries
• Adrenals
• Peripheral fat tissue
• Most important male hormone is testosterone which
  is produced by the testes

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Responsibilities of Testosterone

• Initiating sperm production
• Behavioral characteristics
• Libido
• Sexual potency
• Muscle mass and strength
• Fat distribution
• Bone mass
• Erythropoiesis
• Prevention of baldness

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Hypogonadism

• Deficient hormone production and secretion
• Androgens must be replaced by medications
• May cause virilization, muscle building, and
  hematologic stimulation of erythropoiesis
• Can be used to treat anemia, breast cancer, or
  endometriosis

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Androgens Side Effects

• Virilization
• Hirsutism
• Acne
• Hepatoxicity
• High levels of erythrocytes
• Oily skin
• Gynecomastia
• Priapism

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Male Impotence

• Failure to initiate or maintain an erection until
  ejaculation
• Causes
• Testosterone deficiency
• Alcoholism
• Cigarette smoking
• Psychological factors
• Medications

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Drugs That May Cause Impotence

• Alcohol (most significant)
• Amphetamines
• Antihypertensives
• Corticosteroids
• Estrogens

• H2 blockers
• haloperidol
• lithium
• Opiates
• Some antidepressants

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Agents for Male Impotence
Drug List

• alprostadil (Caverject, Edex, Muse)
• danazol (Danocrine)
• methyltestosterone (Android, Testred)
• oxymetholone (Anadrol)
• papaverine
• testosterone (Androderm, AndroGel, Striant,
  Testoderm)

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Agents for Male Impotence Phosphodiesterase
Inhibitors
Drug List

• sildenafil (Viagra)
• tadalafil (Cialis)
• vardenafil (Levitra)

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sildenafil (Viagra)

• 1st oral therapy for impotence
• Allows an erection to occur naturally
• Take at least 1 hour before activity

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sildenafil Dispensing Issues
Warning!

• Potentially lethal interaction with nitrates

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tadalafil (Cialis)

• Duration of action is 36 hours
• Faster onset and longer duration than others in
  this class

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tadalafil Dispensing Issues
Warning!

• Potentially lethal interaction with nitrates

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Female Hormones

• Can prevent conception, ease symptoms of
  menopause, and help prevent osteoporosis
• 2 main female hormones
• Estrogen
• Progesterone

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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

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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

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Menopause

• As women reach menopause estrogen production
  decreases
• HRT can be used to supplement estrogen levels

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estrogens Dispensing Issues
Warning!

• Patients should not smoke during therapy, whether
  birth control or HRT

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Estrogens Side Effects

• Nausea
• Vomiting
• Bloating
• Weight gain
• Breast tenderness
• Breakthrough bleeding
• Glucose intolerance

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HRT

• Reduces symptoms of menopause
• Decreases bone loss
• Lowers risk of cardiovascular disease
• Small risk of breast cancer

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Estrogens
Drug List

• conjugated estrogen (Enjuvia,Premarin)
• conjugated estrogen-medroxyprogesterone
  (Premphase, Prempro)
• estradiol (Alora, Climara, Esclim, Estrace,
  Estraderm, Estrasorb, Estring, Femring, Menostar,
  Vivelle, Vivelle Dot)

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Estrogens
Drug List

• estradiol-levonorgestrel (Climara Pro)
• estradiol-norethindrone (Activella, CombiPatch)
• estradiol-norgestimate (Ortho-Prefest)

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Estrogens
Drug List

• estropipate (Ogen)
• ethinyl estradiol (Estinyl)
• ethinyl estradiol-norethindrone (Femhrt)

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estrogen-medroxyprogesterone (Premphase, Prempro)

• Provides estrogen and progesterone replacement
• Prevents uterine cancer

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Progestins

• Used primarily in birth control and to prevent
  uterine cancer
• Also used for menstrual dysfunction

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Progestins Side Effects

• Similar to pregnancy
• Weight gain
• Depression
• Fatigue
• Acne
• Hirsutism

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Progestins
Drug List

• levonorgestrel (Norplant II)
• medroxyprogesterone (Depo-Provera, Provera)
• norethindrone (Micronor)

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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

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Benefits of OCs

• 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

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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

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Contraceptive Agents
Drug List

• estradiol cypionate-medroxyprogesterone (Lunelle)
• ethinyl estradiol-desogestrel (Cyclessa, Desogen,
  Kariva, Mircette, Ortho-Cept)
• ethinyl estradiol-drospirenone (Yasmin)

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Contraceptive Agents
Drug List

• estradiol cypionate-medroxyprogesterone (Lunelle)
• ethinyl estradiol-desogestrel (Cyclessa, Desogen,
  Kariva, Mircette, Ortho-Cept)
• ethinyl estradiol-drospirenone (Yasmin)

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Contraceptive Agents
Drug List

• ethinyl estradiol-ethynodiol diacetate (Demulen)
• ethinyl estradiol-etonogestrel (NuvaRing)
• ethinyl estradiol-levonorgestrel (Levlen,
  Nordette, Seasonale, Tri-Levlen, Triphasil,
  Trivora-28)

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Contraceptive Agents
Drug List

• ethinyl estradiol-norelgestromin (Ortho Evra)
• ethinyl estradiol-norethindrone (Estrostep Fe,
  Femhrt, Loestrin Fe, Ovcon)
• ethinyl estradiol-norgestimate (Ortho Tri-Cyclen,
  Ortho Tri-Cylcen Lo)

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Contraceptive Agents
Drug List

• ethinyl estradiol-norgestrel (Lo/Ovral,
  Low-Ogestrel, Ovral)

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ethinyl estradiol-desogestrel (Cyclessa, Desogen,
Kariva, Mircette, Ortho-Cept)

• Inhibits ovulation
• Includes 2 days of placebo followed by 5 days of
  low-dose estrogen
• May be safer for smokers

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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

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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

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ethinyl estradiol-norelgestromin (Ortho-Evra)

• Transdermal contraceptive
• Suppresses gonadotropins
• A new patch is applied every 7 days for 3
  weeks then the 4th week is patch free

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Some Oral Contraceptive Interactions

• Antibiotics
• Anticonvulsants
• Antifungals
• Benzodiazepines
• Bronchodilators
• Corticosteroids
• Lipid-lowering agents
• TCAs

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Emergency Contraception

• In great demand
• Patients want them to be available OTC

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Discussion

• What is one of the arguments for emergency
  contraceptives being OTC?

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Discussion

• What is one of the arguments for emergency
  contraceptives being OTC?
• Answer After making a doctors appointment and
  then going to the get the prescription, sometimes
  it is too late to take the medication

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Contraceptive AgentsEmergency Contraceptives
Drug List

• levonorgestrel (Plan B)
• norgestrel (Ovrette)

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Home Pregnancy Tests

• Critical organ systems develop in the first month
  which is affected by
• Mothers diet
• Environment (smoking)
• Medications
• Consumption of alcoholic beverages

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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

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Drugs Used at Birth

• Often no drugs are necessary for delivery, but in
  some cases they are
• To restart labor
• To decrease uncontrolled bleeding

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Drugs Used at Birth
Drug List

• methylergonovine (Methergine)
• oxytocin (Pitocin)

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oxytocin (Pitocin)

• Natural hormone that stimulates uterine
  contractions
• Drug should be used as a last resort

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oxytocins Side Effects

• For the woman
• Vomiting
• Irregular heart rate
• Tachycardia
• Postpartum bleeding

• For the child
• Bradycardia
• Arrhythmias
• Jaundice

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Sexually Transmitted Disease

• the structural anatomy of the male and female
  genital systems

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Gonorrhea

• Most commonly reported STD
• Caused by Neisseria gonorrhoeae that attaches to
  mucosal cells in
• Oropharyngeal area
• Eye
• Joints
• Rectum
• Male and female genitalia

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Gonorrhea

• If untreated, it can cause systemic infection
  including
• The heart, meninges, eyes, pharynx, and joints
• Eye infections occur most often in newborns and
  can cause blindness

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Syphilis

• Caused by Treponema pallidum
• Incubation averages three weeks
• Infection develops in 3 stages
• Primary stage
• Secondary stage
• Tertiary stage

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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

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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

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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

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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

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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

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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

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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

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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

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Agents for STDs
Drug List

• acyclovir (Zovirax)
• azithromycin (Zithromax)
• ceftriaxone (Rocephin)
• clotrimazole (GyneLotrimin, Mycelex)
• doxycycline (Doryx, Vibramycin)

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Agents for STDs
Drug List

• erythromycin
• fluconazole (Diflucan)
• ketoconazole (Nizoral)
• metronidazole (Flagyl)
• miconazole (Monistat)

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Agents for STDs
Drug List

• penicillin G benzathine (Bicillin L-A)
• spectinomycin (Trobicin)
• tetracycline (Sumycin)
• tioconazole (Vagistat-1)
• valacyclovir (Valtrex)