Lesson 3: Endocrine Pharmacology • Growth-promoting effects mediated by

IGF-1 aka somatomedin C.

1. HYPOTHALAMIC AND PITUITARY
HORMONES GROWTH HORMONE DRUGS

• ANTERIOR PITUITARY HORMONES

a. Growth Hormone (GH)

b. Follicle Stimulating Hormone (FSH)
and Luteinizing Hormone (LH)
c. Prolactin
d. Adrenocorticotropin (ACTH)
e. Thyroid Stimulating Hormone (TSH)

• POSTERIOR PITUITARY HORMONES

a. Oxytocin
b. Vasopressin

ANTERIOR PITUITARY HORMONES

- ALL under the control
HYPOTHALAMIC HORMONE.
Note:
of a
• Somatropin – a GH agonist.
▪ Recombinant Growth Hormone
▪ Increases release of ICG-1 in the
liver and cartilage

USES:

✓ Growth Hormone Deficiency

✓ Genetic Disease associated with short
stature: Turner, Noonan, Prader- Willi

SIDE EFFECTS:

✓ Peripheral Edema
✓ Myalgia
✓ Pseudotumor Cerebri
✓ Slipped Capital Femoral Epiphysis
Note:
• Mecasermin – a GH agonist.
▪ Recombinant IGF -1
A. Growth Hormone (GH) ▪ Stimulates skeletal muscle
growth, amino acids.
• An anterior pituitary hormone
USES:
• Required for attainment of normal adult
size.
 ✓ For CHILDREN UNRESPONSIVE to GH ✓ Gastrinoma
Therapy. ✓ Variceal Bleeding

SIDE EFFECTS: SIDE EFFECTS:

✓ Hypoglycemia ✓ Gastrointestinal Disturbances

✓ Arrhythmias
✓ Gallstones

B. GONADOTROPINS (FSH & LH)

• An anterior pituitary hormone

• Gonadotropins - are produced by

GONADOTROPH cells.

• Serve COMPLEMENTARY functions in

the reproductive process.

• FSH & LH - are used for OVARIAN

steroidogenesis.

• FSH - is mainly for FOLLICLE

development in women,
spermatogenesis in men.
Note: • LH - stimulates ANDROGEN production.
• Pegvisomant – a GH antagonist. GONADOTROPINS DRUGS
▪ Block GH receptor.

USES:

✓ Acromegaly

SIDE EFFECTS:

✓ Diarrhea
✓ Nausea
✓ Elevated LFTs

• Octreotide & Lanreotide – a GH

antagonist.
▪ Suppress the release of growth
hormones.

USES:

✓ Acromegaly
✓ Pituitary Adenoma
✓ Carcinoid
Note:

• Follitropin Alfa – a preg cat x.

▪ Activates FSH receptor.
▪ Mimics effects of FSH.
Note:
USES:

✓ Controlled ovarian hyperstimulation • Leuprolide – a preg cat x.

✓ Infertility ▪ Agonist of GnRH receptors.
▪ Increased LH and FSH secretion
SIDE EFFECTS: with INTERMITTENT
administration.
✓ Headache
▪ Reduced LH and FSH secretion
✓ Depression
with PROLONGED continuous
✓ Edema
administration.
✓ Ovarian Hyperstimulation Syndrome
USES:
• Choriogonadotropin Alfa – a preg cat x.
✓ Ovarian Suppression
▪ Activates LH receptors.
✓ Myoma Uteri
▪ Mimics effects of LH.
✓ Central Precocious Puberty
SIDE EFFECTS: • Anti-Diuretic Hormone / Vasopressin
(ADH)
✓ Hot flushes
✓ Sweats • Are synthesized in neuronal cell bodies
✓ Headache in the hypothalamus and transported
✓ Gynecomastia via their axons to the posterior pituitary,
where they are stored and then released
C. PROLACTIN
into the circulation.
• An anterior pituitary drug.
• Each has LIMITED but important clinical
• Principle hormone responsible for uses.
LACTATION.
OXYTOCIN

• is a peptide hormone secreted by the

posterior pituitary.

• stimulates muscular contractions in the

uterus and myoepithelial contractions in
the breast.

• Responsible for “MILK-LET-DOWN”

Note:

• Bromocriptine – a preg cat B.

▪ Inhibits prolactin release from
the pituitary gland.

USES:

✓ Hyperprolactinemia
✓ Pituitary Adenoma
✓ Acromegaly
Note:
✓ Parkinson’s Disease

SIDE EFFECTS: • Oxytocin – activates oxytocin receptors.

✓ Erythromelalgia – rare disorder USES:

characterized by BURNING PAIN and ✓ Labor Induction
WARMTH and REDNESS of the ✓ Labor augmentation
extremities. ✓ Control of postpartum hemorrhage
POSTERIOR PITUITARY HORMONES SIDE EFFECTS:
• Oxytocin ✓ Fetal distress
✓ Placental abruption
• Atosiban - oxytocin receptor blocker. Note:

ANTI-DIURETIC HORMONE (ADH) / • Vasopressin and Desmopressin – a ADH

VASOPRESSIN agonist.
▪ Selective for v2 receptors.
• Vasopressin - is a peptide hormone
released by the posterior pituitary in USES:
response to rising plasma tonicity or
✓ Central Diabetes
falling blood pressure.
SIDE EFFECTS:
• It possesses antidiuretic and vasopressor
properties. ✓ GI disturbance
✓ Headache
• A deficiency of this hormone results in
✓ Flushing
DIABETES INSIPIDUS.

• Diabetes insipidus - is a syndrome of • Conivaptan – a ADH antagonist.

polyuria, polydipsia, and hypernatremia. ▪ Antagonist at v1a and v2
receptors.
▪ Excessive urination due to
kidney’s inability resorb water USES:
properly from urine.
✓ SIADH

SIDE EFFECTS:

✓ Infusion site reactions

✓ Hyperkalemia

2. THYROID AND ANTITHYROID DRUGS

KEY FEATURES OF HYPERTHYROIDISM AND

HYPOTHYROIDISM
 USES:

✓ Hypothyroidism
✓ Myxedema coma

SIDE EFFECTS:

✓ Dry skin
✓ Sweating
✓ Tachycardia
✓ Nervousness
✓ Tremor

HYPERTHYROIDISM
HYPOTHYROIDISM
• aka Thyrotoxicosis.
• Is a syndrome resulting from deficiency
of thyroid hormones and is manifested • Is a result of HIGH LEVELS of thyroid
largely by a reversible slowing down of hormone.
all body functions.
• Most COMMON FORM is called GRAVE’S
• Hypothyroidism - can occur WITH OR DISEASE or diffuse toxic goiter.
WITHOUT thyroid enlargement (goiter).
• Laboratory diagnosis is high T3, T4, FT3,
• The laboratory diagnosis of FT4, and low serum TSH.
hypothyroidism in the adult - is easily
DRUGS FOR HYPERTHYROIDISM
made by the combination of low free
thyroxine and elevated serum TSH levels

• MYXEDEMA COMA – a result of

untreated hypothyroidism; medical
emergency.

Note:

• Levothyroxine – thyroid hormone.

▪ Activation of nuclear receptors.
Note:

• Propylthiouracil – thioamide.
▪ Inhibits thyroid peroxidase
reactions.

USES:

✓ Hyperthyroidism
✓ Thyroid Storm

SIDE EFFECTS:

✓ Agranulocytosis

• Methimazole – thioamide.
▪ Inhibits thyroid peroxidase
reactions.

• Radioactive Hormone – iodine.

▪ Administered orally in solution
as sodium.

USES:

✓ Hyperthyroidism

Note:

• Potassium Iodide – iodine.

▪ Inhibits iodine organification

and hormone release.

USES:

✓ Hyperthyroidism

• Propranolol – beta blocker.

▪ Blocks beta – receptors.

Note:

• Propylthiouracil – drug choice for

PREGNANT HYPERTHYROID Px.
▪ Preferable during first trimester.
Note:
▪ Shorter DOA
▪ FASTEST onset action. • Iodine – preferred for MOST patients.
▪ PERMANENT cure of
• Methimazole – drug choice for Thyrotoxicosis.
NONPREGNANT HYPERTHYROID Px. ▪ CONTRAINDICATED in pregnant
▪ Causes Aplasia Cutis Congenita women.
▪ Thiamazole – another name of • Potassium Iodide – should NOT used
methimazole. alone.
▪ SLOWEST onset action.
 GLUCOCORTICOID RELATED DRUGS

Note:

• Propanolol – use beta blockers

WITHOUT intrinsic sympathomimetic
activity.

I. ADRENAL CORTICOSTEROID DRUGS

Note:
• Major groups are:
GLUCOCORTICOIDS: (short acting, low potency)
1. MINELAROCORTICOIDS
LOW MEDIUM HIGH
2. GLUCOCORTICOIDS
POTENCY POTENCY POTENCY
Hydrocortisone Fluticasone Desoximetasone
• Mineralocorticoids – regulates sodium – prototype
and potassium reabsorption in the
collecting tubules of kidney.
• Betamethasone – HIGHEST anti-
• Glucocorticoids – important effects on inflammatory potency.
metabolism, catabolism, immune GLUCOCORTICOIDS: (intermediate to long
responses, and inflammation. acting, medium to high potency)
 • Prednisone – suppresses inflammation USES:
and immune response.
✓ Cushing Syndrome
▪ Wide variety of inflammatory.

• Mifepristone – glucocorticoid
antagonist.
▪ Competitive inhibitor at the GC
receptor.

USES:

✓ Cushing’s Syndrome

CUSHING’S SYNDROME

• Syndrome caused by ANY condition that

produces elevated glucocorticoid levels.

Note:

• Amino Glutethiamide – glucocorticoid

synthesis inhibitor.
▪ Desmolase inhibitor.
▪ Inhibits Desmolase blocking.

USES:

✓ Breast cancer
✓ Cushing Syndrome
MINERALOCORTICOID RELATED DRUGS

• Ketozonazole – glucocorticoid synthesis

inhibitor.
▪ CYP450 inhibitor.
▪ Inhibits cholesterol sidechain
cleavage.

USES:

✓ Adrenal carcinoma
✓ Hirsutism

• Metyrapone – glucocorticoid synthesis

inhibitor.
▪ 11-B hydroxylase inhibitor.
▪ Inhibitor of steroid 11-
hydroxylation.
Note: INSULIN

• Fludrocortisone – strong agonist of • Synthesized as prohormone proinsulin.

mineralocorticoid AGONIST receptor.
• Cleavage of proinsulin and cross-linking
USES: result in formation of insulin and a
residual C-peptide.
✓ Adrenalectomy
• C-peptide - is used to DIFFERENTIATE
SIDE EFFECTS:
type 1 and type 2 DM.
✓ Salt & Fluid retention
Note: MOA - binds to a tyrosine kinase
✓ Hypokalemia
receptor.
✓ Congestive Heart Failure

• Spironolactone – mineralocorticoid
ANTAGONIST.
▪ Blocks aldosterone receptors.

USES:

✓ Heart failure
✓ Hypokalemia

SIDE EFFECTS:

✓ Gynecomastia

ANTIDIABETIC DRUGS

• DIABETES MELLITUS - chronic disorder

of carbohydrate, fat, and protein
metabolism due to a relative or absolute
deficiency in insulin secretory response.

• TYPE 1 DIABETES - usually has its onset

during childhood and results from auto
INSULIN SECRETAGOGUES (NON-INSULIN
immune destruction of pancreatic b
AGENTS)
cells: NO C-PEPTIDE.
• Stimulate the release of endogenous
• TYPE 2 DIABETES - progressive disorder
insulin by promoting closure of
characterized by increasing insulin
potassium channels in the pancreatic B-
resistance.
cell membrane.
▪ frequently associated with
• Depolarizes the cell and triggers insulin
obesity and is much more
release.
common than type 1 diabetes.
• NOT effective in patients who LACK
▪ usually has its onset in functional pancreatic B cells.
adulthood; HAS C-PEPTIDE.
 INSULIN SENSITIZERS

Note:

• Chlorpropamide – preg cat C.

▪ Secretagogues.
▪ 1st generation Sulfonylurea.
▪ Increases Insulin secretion from
Note:
pancreatic beta cells by closing
ATP SENSITIVE K+ channels. • Metformin – sensitizers.
▪ Biguanide.
USES:
▪ Activates AMP - stimulated
✓ Type 2 diabetes mellitus protein kinase.

SIDE EFFECTS: USES:

✓ Hypoglycemia ✓ DRUG CHOICE for Obese Diabetics.

✓ Weight gain
SIDE EFFECTS:
✓ Hyperemic Flush
✓ Lactic acidosis
• nd
Glipizide – 2 generation sulfonylurea.
▪ Increases Insulin secretion from • Pioglitazone – sensitizers.
pancreatic beta cells by closing ▪ Binding to PPAR – gamma and
ATP SENSITIVE K+ channels. PPAR – alpha.

USES: USES:

✓ Type 2 diabetes mellitus. ✓ Type 2 diabetes mellitus

SIDE EFFECTS: SIDE EFFECTS:

✓ Hypoglycemia ✓ Fluid retention

✓ Photosensitivity ✓ Anemia
✓ Weight gain
• Meglitinide - Increases Insulin secretion
from pancreatic beta cells by closing
ATP SENSITIVE K+ channels.

USES:

✓ Type 2 diabetes mellitus.

 OTHER NON-INSULIN DRUGS ✓ Hypoglycemia
✓ Acute pancreatis

• Sitagliptin – incretin modulator.

▪ DPP-4 inhibitor.
▪ Inhibits dipeptidyl peptidase.

USES:

✓ Type 2 diabetes mellitus

SIDE EFFECTS:

✓ Headache
✓ Nasopharyngitis
✓ Upper respiratory tract

Note: • Dapagliflozin – SGLT2 inhibitor.

• Acarbose – alpha-glucosidase inhibitor. ▪ NA-Glucose CO-Transporter 2
▪ Inhibits intestinal a- glucosides. inhibitor.

USES: USES:

✓ Type 2 diabetes mellitus ✓ Type 2 diabetes mellitus

SIDE EFFECTS: WOMEN’S HEALTH

✓ Gastrointestinal disturbance 1. Estrogen

2. Birth Control
3. Drug Therapy and Infertility
4. Drug affecting uterine contraction
• Pramlintide – amylin analog.
▪ Activates amylin receptors. ESTROGEN
USES: • Estradiol – major ovarian estrogen in
women.
✓ Type 1 and Type 2 diabetes mellitus

SIDE EFFECTS: • Synthetic estrogens with high

bioavailability such as:
✓ Hypoglycemia
✓ Gastrointestinal disturbances
1. Ethinyl estradiol
2. Mestranol
• Exenatide – incretin modulator.
▪ Activates GLP-1 receptors.
• Ethinyl Estradiol & Mestranol –
USES: used as HORMONAL contraceptives.

✓ Type 2 diabetes mellitus

SIDE EFFECTS:
 ▪ Activates estrogen
receptors.

USES:

✓ Atrophic vaginitis
✓ Hormone replacement

• Ethinyl estradiol & Diethylstilbestrol

SIDE EFFECTS:

✓ Migraine
✓ Thromboembolism

PROGESTINS

Note:
Note:
• Ethinyl estradiol – estrogen.
• Norgestrel – activates progesterone
• Premarin – from PREgnant MARe’s
receptors.
urine.
▪ Activates estrogen HORMONAL CONTRACEPTIVES
receptors.
• Contain EITHER a combination of an
USES: estrogen and a progestin or a progestin
alone.
✓ Primary hypogonadism
✓ Postmenopausal Hormonal • Available in a variety of preparation.
✓ Replacement Therapy
▪ Oral Pills
• Diethylstilbestrol - synthetic estrogen ▪ Long-Acting Injections (Good
(NONSTEROIDAL). For 3 Months)
▪ Implants (Good For 3 Years)
▪ Transdermal Patches
 ▪ Vaginal Rings ▪ prevent pregnancy if
▪ Intrauterine Devices (IUDS) administered within 72 h after
unprotected intercourse.
MOA OF COMBINATION HORMONAL
CONTRACEPTIVES
▪ progestin (L-Norgestrel) alone,
• Inhibition of ovulation (the primary estrogen alone, combination of
action). estrogen and progestin.

• Effects on the cervical mucus glands, ▪ progestin-only preparation

uterine tubes. causes fewer side effects than
• Endometrium that decreases the the estrogen-containing
likelihood of fertilization and preparations.
implantation. 2. CONTRACEPTIVES
TYPES OF ORAL CONTRACEPTIVE

1. MONOPHASIC

▪ combination estrogen-progestin
tablets that has a constant
dosage throughout the
menstrual cycle.
Note:
2. BIPHASIC or TRIPHASIC
• Estradiol + Norethindrone – combined
▪ combination preparations in oral contraceptive.
which the progestin or estrogen USES:
dosage, or both, changes during
the month ✓ Contraception
✓ Hypogonadism
▪ more closely mimics hormonal ✓ Acne
changes in menstrual cycle.
SIDE EFFECTS:

✓ Breakthrough bleeding
3. PROGESTIN-ONLY PREPARATIONS ✓ Nausea

▪ recommended for breastfeeding • Medroxy - progesterone acetate –

moms since they do not affect progestin - only contraceptive.
lactation ▪ Activates progesterone
receptors.
4. Postcoital Contraceptives / Emergency
Contraception USES:

✓ Contraception
✓ Hormone replacement therapy
SIDE EFFECTS: ✓ For patients with HISTORY of Breast
Cancer in the management of hot
• Levonorgestrel – postcoital
flushes.
contraceptive.
▪ Activates estrogen and or
• Clomiphene – partial agonist of estrogen
progesterone receptors.
receptors in pituitary.
USES:
USES:
✓ Emergency contraception

SIDE EFFECTS:
✓ Antagonist to estrogen receptors in the
✓ Severe nausea pituitary
✓ Vomiting
SIDE EFFECTS:
✓ Breast Tenderness
✓ Hot flushes
✓ Eye symptoms (afterimages)
SELECTIVE ESTROGEN RECEPTOR
MODULATORS (SERMS)

Note:

• Tamoxifen – estrogen antagonist actions

in breast tissue and CNS.

USES:

✓ For BREAST cancer patients who are ER

+ PR +

SIDE EFFECTS: Note:

✓ Hot flushes • Anastrozole – aromatase inhibitor.
✓ Thromboembolism ▪ Enzyme which converts
testosterone to estrogen.
• Raloxifene – estrogen antagonist actions
in breast tissue and CNS. USES:

USES: ✓ Breast cancer

✓ Precocious Puberty

SIDE EFFECTS:
 ✓ Hot flushes INFERTILITY DRUGS (SERM)
✓ Musculoskeletal disorders
✓ Osteoporosis

• Danazol – ovarian inhibitor.

▪ Weak cytochrome P450
inhibitor.

USES:

✓ Endometriosis
✓ Fibrocystic disease

SIDE EFFECTS:

✓ Acne
✓ Hirsutism
✓ Weight gain
INFERTILITY DRUGS (GONADTROPIN)

• Leuprolide – preg cat X.

▪ GnRH agonists.

USES:

✓ Ovarian suppression
✓ Controlled ovarian hyperstimulation

SIDE EFFECTS:

✓ Hot flushes
✓ Sweats
✓ Headache

• Ganirelix – GnRH antagonist.

▪ Reduces endogenous
production of LH and FSH.

• Mifepristone (RU 486) – Glucocorticoid

and Progesterone receptor antagonist.

3. INFERTILITY DRUGS

If a couple has NOT BEEN able to conceive

within a reasonable period, doctor’s
Note:
evaluation will be needed.
Couples will be tested with regards to their • Follitropin Alfa – FSH analog.
fertility.
USES:
 ✓ Controlled ovarian
✓ Hyperstimulation
INFERTILITY DRUGS
SIDE EFFECTS:

✓ Headache
✓ Depression
✓ Edema
✓ Ovarian Hyperstimulation

• Choriogonadotropin Alfa – LH analog.

USES:

✓ Initiation of ovulation during controlled

ovarian hyperstimulation.

SIDE EFFECTS:

✓ Headache
✓ Depression
✓ Edema

INFERTILITY DRUGS (INSULIN

SENSITIZER/BIGUANIDE)

Note: Works SAME as clomiphene. Usually used

for women younger than 39 who have PCOS.

Note: Given when insulin resistance is a known

or suspected cause of infertility - usually in
women with PCOS.

Note: Used when ovulation problems are caused
by excess production of prolactin.
• Hyperprolactinemia – excess
production of prolactin.
SURGERIES TO RESTORE FERTILITY
1. LAPARASCOPIC OF HYSTEROSCOPIC
SURGERY – to correct problems with
uterine anatomy, removing endometrial
polyps, or removing pelvic or uterine
adhesions.
2. TUBAL SURGERIES – can be done if your
fallopian tubes are blocked or filled with
fluid.
3. INTRAUTERINE INSEMINATION –
millions of healthy sperm will be placed
inside the uterus around the time of
ovulation.
4. ASSISTED REPRODUCTIVE
TECHNOLOGY (IVF) – involves retrieving
mature eggs, fertilizing them with sperm
in a dish in a lab, then transferring it to
the uterus after.
RISKS OF FERTILITY DRUGS
• Pregnancy with multiples
• Ovarian Hyperstimulation Syndrome
• Long-term risk of ovarian tumors
4.DRUGS AFFECTING UTERINE FUNCTION
 • Use for labor induction, labor
augmentation, control of postpartum
hemorrhage.

ERGOT ALKALOID (ERGONOVINE and

METHYLERGONOVINE)

• Uteroselective serotonin receptor

antagonist.

• Used for post-partum bleeding.

• Should never be given before the

PROSTAGLANDIN E2 ANALOG delivery of placenta.
(DINOPROSTONE)
B2-ADRENOMIMETICS (FENOTEROL)
• Low concentrations contract, higher
concentrations relax uterine and cervical • Causes uterine relaxation
smooth muscle, soften cervix at term
before induction with oxytocin. • Stops premature labor

▪ Used for Induction of labor (Cervical • DOES NOT cause any negative effects to
ripening), Abortifacient. the fetus.
▪ Side effects include cramping and
fetal trauma. • Contraindicated in patients with cardiac
defects:
• Approved abortifacient in the 2nd ▪ Arrythmia
trimester. ▪ Glaucoma
▪ Thyrotoxicosis
• Although effective in inducing labor, it
B2-ADRENOMIMETICS (MAGNESIUM SULFATE)
produces more SE than other oxytocics.
• Decreases uterine contraction
PROSTAGLANDIN F2A ANALOG (CARBOPROST) • Acts as a CALCIUM ANTAGONIST
• Also possess hypotensive effects
- Activates FP receptor.
MENS HEALTH
- Control of postpartum hemorrhage, for
refractory postpartum bleeding, 1. Androgens
abortifacient. 2. Drugs for Erectile Dysfunction
3. Drugs for Benign Prostatic Hyperplasia
OXYTOCIN
1. ANDROGENS
• Activates oxytocin receptors.
TESTOSTERONE
• Stimulates uterine contraction and
labor. • synthesized from progesterone and
dehydroepiandrosterone (DHEA)
 ▪ Increased by estrogen, thyroid ANTI – ANTOGENS
hormone, and cirrhosis.

▪ Decreased by androgen, growth

hormone and obesity.

▪ Converted in several organs

Example: prostate to dihydrotestosterone

(DHT), which is the active hormone in those
tissues. Note:

• Flutamide – androgen receptor

antagonist.
▪ Competitive antagonist.

USES:

✓ Prostate cancer
✓ Surgical castration (NILUTAMIDE)

SIDE EFFECTS:

✓ Gynecomastia
✓ Hot flushes

Note: • Cyproterone – antagonist at androgen

receptor.
• Testosterone – androgens.
▪ Promotes development of male USES:
characteristics.
✓ Hirsutism
USES: ✓ Decreases sexual drive-in men
✓ Male hypogonadism SIDE EFFECTS:
SIDE EFFECTS: ✓ Hepatotoxicity
✓ Adrenal suppression
✓ Paradoxical feminization may be due to
✓ Depression
negative feedback on physiologic
testosterone level.
• Finasteride – FinAsteRide (Five Alpha
Reductase Inhibitor)
▪ Dihydrotestosterone – most
POTENT form of testosterone.

USES:

✓ Giving 5 – alpha reductase aids in

management of smooth muscle
hypertrophy in the prostate.
 SIDE EFFECTS: What drugs can CAUSE PRIAPISM?

✓ Gynecomastia “Tigas PeniS Qo, AyaW Bumaba!”

✓ Depression
Trazodone Alprostadil
DRUGS FOR ERECTILE DYSFUNCTION Papaverine Warfarin
Sildenafil Bupropion
Quetiapine

3. DRUGS FOR BENIGN PROSTATIC

HYPERPLASIA

1. ALPHA 1- BLOCKER (PRAZOSIN)

PROSTAGLANDIN E-1 ANALOG (ALPROSTADIL) 2. Blocks a1 receptors
3. Tamsulosin: most SELECTIVE for
• Activates EP receptors, causes vascular prostatic smooth muscle.
smooth muscle relaxation and
vasodilation

• Used for erectile dysfunction.

▪ Given as injection into the

cavernosa.

PHOSPHODIESTERASE 5 INHIBITOR
(SILDENAFIL)

• Inhibits PDE5 which degrades cGMP to

inactive GMP → vasodilation.

• DO NOT take with Nitrates (ISDN, ISMN,

NTG) because it may lead to fatal
hypotension.

• Used for erectile dysfunction.

DRUGS THAT CAN CAUSE ERECTILE

DYSFUNCTION

What drugs can CAUSE erectile dysfunction?

“A SORE PeniS can’t Fuck Hard!”

SSRIs Propranolol
Opiates Spironolactone
Risperidone Finasteride
Ethanol, Estrogen Hydrochlorothiazide