HTHSCI 2H03 - Medications

Growth Hormone/Somatotropin Agonist - Purpose

Treat GH deficiency (induce

growth)

Growth Hormone/Somatotropin Agonist - MOA

Mimics full effects of somatotropin = Increased muscle mass, bone density, protein synthesis, etc.

Growth Hormone/Somatotropin Agonist - SE/AE

- GH hypersecretion = Causes

- tumours

- acromegaly (rapid tissue growth)

- Fatigue

- Sweating

Growth hormone antagonist - Purpose

Improve/reverse acromegaly

Growth hormone antagonist - Types - Listed

1. Octreotide (slower acting)

2. Pegivosmant (rapid effect)

Growth hormone antagonist - SE/AE

- GH hyposecretion

- Less growth, decreased bone

density (osteoporosis, risk of CV) and muscle mass

- Central adiposity

- dyslipidemias

Growth hormone antagonist - Types - Octreotide (slower acting) -MOA

Binds to GHIH receptors to mimic GHIH = INHIBIT GH secretion

Growth hormone antagonist - Types - Pegivosmant (rapid effect) - MOA

Binds to INHIBIT GH receptors = loss

of effect

ADH agonist - Purpose

Increase renal water reabsorption to treat ADH deficiency

ADH agonist - Types - Listed

1. Desmopressin (partial agonist)

2. Vasopressin

ADH agonist - Types - Desmopressin (partial agonist) - MOA

- Mimics ADH effects: conserve 90%

water

- Increases BP via Water Conservation NOT vasoconstriction

ADH agonist - Types - Vasopressin - MOA

- Little antidiuretic effect

- Potent vasoconstrictor

ADH agonist - SE/AE

Dose too high= Water retention =

increase in BP + weight

Thyroid hormone agonist - Purpose

Reverses effects of hypothyroidism

- Increased

metabolism

- Weight loss,

Increased temp, activity and pulse

Thyroid hormone agonist - Types + Explained

Levothyroxine

- Synthetic T4

- T4 to T3 conversion to restore thyroid hormone function

Thyroid hormone agonist - SE/AE

Hyperthyroidism since making TOO much T3/T4

Thyroid hormone agonist - Clinical Notes + Dosage

Narrow therapeutic index, monitor

- Serum TSH levels

Levothyroxine: PO 1x daily

Thyroid hormone antagonist - Purpose

Reverses effects of hyperthyroidism

Thyroid hormone antagonist - Types - Listed

1. Propylthiouracil and methimazole

2. Sodium Iodide-131 (radioactive iodine)

Thyroid hormone antagonist - Propylthiouracil and methimazole - MOA

- Inhibit T3, T4 synthesis

- Disrupts TSH to T3, T4 conversion

- Takes 3-4w for effect

Thyroid hormone antagonist - Sodium Iodide-131 (radioactive iodine) - MOA

Permanent destruction of T3, T4

- Single admin

Thyroid hormone antagonist - SE/AE

Hypothyroidism

- For Radioactive iodine: too

much thyroid cells

destroyed

Glucocorticoids (cortisol) - Purpose

Treat inflammation

- Metabolism, catabolism

- Suppress immune and inflammatory responses

- Prescribed to treat adrenal insufficiency

- Increased glucose levels, lipid breakdown

- Increase vascular SM sensitivity to NE and angiotensin 2

- Mood, CNS excitability, decreased bone density, bronchodilation

Glucocorticoids (cortisol) - SE/AE

- Changes in moods: aggression, depression

- Immune and inflam

suppression

- Adrenal Atrophy if TOO MUCH

Corticosteroids (glucocorticoids + mineralocorticoids) - Purpose

- Immune suppression

- Myopathy

- Osteoporosis

- Mood changes

- Edema

- Hypertension

- Hyperglycemia

- Fluid retention

- Hyperlipidemia

- F and E imbalances

Corticosteroids (glucocorticoids + mineralocorticoids) - Absorption

Well absorbed and distributed, highly bound to plasma proteins

Corticosteroids (glucocorticoids + mineralocorticoids) - Metabolism

Metabolized in liver, excreted by kidneys

Corticosteroids (glucocorticoids + mineralocorticoids) - RE: Pregnancy

Crosses placenta and enters breast milk:

Combination oral contraceptives - Purpose

Inhibit ovulation

Combination oral contraceptives - Synthetic Progestin - MOA

- Produce thin + inactive endometrium: implantation impossible

- Thick cervical mucus: prevent sperm movement

Combination oral contraceptives - Benefits

- Reduced PMS symptoms

- Reduced risk of certain cancers

- Decreased risk of ovarian cysts and endometriosis

- Improvements in bone mineral density and acne

Combination oral contraceptives - AE - Estrogen

- inhibits breast milk

- breast tenderness

- edema

- nausea

Combination oral contraceptives - Progestin

- Hirsutism (male hair patterns)

- Increased blood glucose

- hypertension

- Increased appetite = weight gain

- depression

- Acne

- Fatigue

- Thromboembolic disorders (smokers, 35+)

Combination oral contraceptives - Contraindications

- Breast cancers + tumours

- Hepatic cirrhosis (renal + liver dysfunction),

- immobilization

- aura migraines

- Smoking + stroke history

Combination oral contraceptives - Caution

- Depression

- Hypertension

- Diabetes

Progestin only contraceptives - Reliability

Not as reliable in ovulation inhibition

Progestin only contraceptives - Effects

- Thin + inactive endometrium (prevents implantation)

- Thick cervical mucus (prevents sperm movement)

- Endometrium is kept in atrophic state to inhibit zygote implantation

Progestin only contraceptives - Benefits

Good for women who cannot handle SE of combination contraceptives (smokers, hypertensive, breast feeding)

Progestin only contraceptives - AE

- Menstrual irregularities (amenorrhea, prolonged bleeding, breakthrough spotting)

- Risk of ovarian cysts and cancer

- Increased appetite, weight gain

- Fatigue

- Depression

- Acne

- Headaches

Emergency contraceptive (Plan B) - Purpose

Prevents unplanned pregnancy related to unprotected sexual intercourse or contraceptive failure

via INHIBITING ovulation

Emergency contraceptive (Plan B) - SE

- Nausea

- Vomiting (take gravol to treat)

- Dizziness, headache, fatigue

- Diarrhea

- Abdominal pain, breast tenderness

- May induce menstrual bleeding (not menstrual period)

Abortifacients - Purpose

used to terminate an unwanted pregnancy up to gestational age of 63 days (measured based on LMP)

Abortifacients - Types + Composed of...

Mifegymiso (RU 486)

- Involves two drugs

1. Mifepristone

2. Misoprostol

Abortifacients - Mifepristone - MOA

Progesterone receptor MODULATOR: BLOCKS effects of progesterone on endometrium and myometrium (progesterone antagonist)

Allows for misoprostol action

Abortifacients - Misoprostol - MOA

Progesterone AGONIST: INDUCES uterine contractions, allowing embryo to be expelled

Hormone replacement therapy (old version) - Purpose

Relieves menopause symptoms

- Insomnia

- Hot flashes

- Vaginal atrophy

- Mood disturbances

- Irritability

- Osteoporosis

Hormone replacement therapy (old version) - MOA

Estrogen + progestin HRT

Hormone replacement therapy (old version) - SE

Increase risk in

- MI

- Stroke

- Breast cancer

- Dementia

- DVT women 60+

Hormone replacement therapy (duavive) - Purpose

Manges symptoms of menopause AND Reduces risk of menopause-induced osteoporosis

Hormone replacement therapy (duavive) - Composition

Estrogen + bazedoxifene (a SERM/selective estrogen receptor modulator)

Hormone replacement therapy (duavive) - MOA

Bazedoxifene ANTAGONIZES effects of estrogen on uterus= reduces risk of uterine cancers

Bazedoxifene AGONIZES bone activity (pro bone), also allows other estrogen effects

Hormone replacement therapy (duavive) - SE/AE

- Muscle spasms

- Nausea, diarrhea, upset stomach

Abdominal, throat, neck pain

- Dizziness

- THromboembolism risk (always with estrogen)

Insulin therapy - Basal - Purpose

CLOUDY background insulin to mimic hepatic glucose production

- For T1DM

Insulin therapy - Bolus - Purpose

CLEAR secreted in response to sudden burst of energy (ie. intake and glucose via food)

- For T1DM

Insulin therapy - Basal - MOA

Rapid acting: after meals

Short acting: before meals

Insulin therapy - Bolus - MOA

Intermediate acting: takes between short to long to activate

Long acting insulin: long activation

Insulin Therapy - SE/AE

Hypoglycemia on short acting insulin

Metformin - Purpose

Monotherapy to enhance insulin sensitivity in peripheral tissues

- T2DM + LOWERS blood glucose

Metformin - MOA

Activates AMP-activated protein kinase (cAMP >> pKA)

Metformin - SE/AE

- GI concerns

- Hepatic or renal failure (lactic acidosis)

- HYPOglycemia

GLP-1 receptor agonists - Purpose + MOA

- T2DM + LOWERS blood glucose

- Incretin pathway activation= in insulin INCREASE and DECREASE in glucagon (lowers blood glucose)

GLP-1 receptor agonists - AE/SE

- Thyroid disorders (ie. cancers, endocrine neoplasia syndrome, parafollicular cell hyperplasia)

- Pancreatitis

- Hypoglycemia

SGLT2 inhibitors - Purpose + MOA

- T2DM + LOWERS blood glucose

INHIBITS renal glucose reabsorption

SGLT2 inhibitors - AE/SE

- Polyuria

- Increase genital and UTI (sugar and urine don't mix, high risk in senior F)

- HYPOglycemia

DPP-4 inhibitors - Purpose + MOA

- T2DM + LOWERS blood glucose

Binds and inhibits DPP-4 receptors

DPP-4 = CAN'T breakdown incretin = INCREASED insulin, DECREASED glucagon

DPP-4 inhibitors - SE/AE

- Pancreatitis

- HYPOglycemia

Insulin - Purpose + MOA

- T2DM + LOWERS blood glucose

Activation of insulin receptors = Regulates metabolism of carbs, fat, protein

Insulin - SE/AE

- Weight gain

- Hypoglycemia

Thiazolidinedizones - MOA - Purpose

- T2DM + LOWERS blood glucose via INCREASING insulin sensitivity in peripheral tissues

Thiazolidinedizones - MOA

Activation of peroxisome proliferator activated gamma receptors in the liver = insulin sensitization and glucose metabolism

Thiazolidinedizones - SE/AE

- Weight gain

- Edema

- Major issue: CHF

- Fractures

Alpha-glucosidase inhibitors - Purpose + MOA

INHIBITS pancreatic alpha-amylase and alpha-glucosidase for starch --> glucose conversion = lower blood glucose

- T2DM + LOWERS blood glucose

Alpha-glucosidase inhibitors - AE/SE

- GI (since it acts on digestive system)

- Gas, diarrhea

- Hypogylycemia

Insulin secretagogues: sulfonylurea and meglitinide - Purpose + MOA

Activates sulfonylurea receptor on beta cell to INCREASE insulin secretion

- T2DM + LOWERS blood glucose

Insulin secretagogues: sulfonylurea and meglitinide - AE/SE

- Weight gain

- Renal/hepatic issues

TOXIC for elderly; OVERWORKS pancreas

Antiobesity agent - Purpose + MOA

Inhibits lipase = insulin become more sensitive = decline in blood glucose

Antiobesity agent - AE/SE

- GI associated with increased fat intake

- Diarrhea

Oxytocin Agonist - Purpose

Augmentation of labour: Increase frequency and force of uterine contractions

Oxytocin Agonist - MOA

Gq Coupled Protein Receptors stimulated = increased IP3 >> binds to sarc ret = increase Ca2+

Oxytocin Agonist - AE/SE

- Uterine HYPERTONUS

- Binding to ADH receptors = antidiuretic effect (pulmonary edema, heart failure, water intoxication)

Oxytocics - Prostaglandin agonist - Purpose

Initiation of labour + postpartum hemorrhage

Oxytocics - Prostaglandin agonist - Types + Notable one

- Dinoprostone

- Carboprost

- Misoprostol (FOR ABORTION)

Oxytocics - Prostaglandin agonist - MOA

- Gq stimulation = more IP3 = more Ca2+

- Gi stimulation: decreases cAMP concentration = less phosphorylation of Ca2+ using-proteins = more Ca2+ for contractions

Oxytocics - Prostaglandin agonist - AE/SE

- Hypertension

- Bronchospasm

- Nausea, vomiting, diarrhea, headache

Oxytocics - Prostaglandin agonist - Contraindications

- Previous C-Section

- Past uterine hypertonus

- Combination w/ other oxytocics

Oxytocics - Prostaglandin agonist - Notes

Do not use for augmentation of labour

Oxytocics - Ergot alkaloids - Purpose

Management of postpartum hemorrhage

Oxytocics - Ergot alkaloids - MOA

Binds to GQ protein coupled prostaglandin E1 receptors and alpha-1 adrenoreceptors = CONTRACTION of muscle in uterus and vasculature

Oxytocics - Ergot alkaloids - SE/AE

Due to alpha-1 adrenoceptor binding: causes high BP/hypertension risk

Oxytocics - Ergot alkaloids - Notes

NOT for contraction = uterine hypertonus risk

ONLY for postpartum hemorrhage

Tocolytics - Prostaglandin inhibitors (NSAIDs) - Purpose

Preterm labour PREVENTION

Tocolytics - Purpose

- Relax uterus for glucocorticoid admin

- Delivery at facility with neonatal ICU

- Treat underlying self limiting conditions that are unlikely to cause recurrent preterm labour

Tocolytics - Prostaglandin inhibitors (NSAIDs) - MOA

- Inhibits COX1 and COX2 enzymes = STOP prostaglandin generation = labour delay and anti-inflammation

Tocolytics - Prostaglandin inhibitors (NSAIDs) - AE/SE - Maternal

- Nausea

- Increased risk postpartum hemorrhage

Tocolytics - Prostaglandin inhibitors (NSAIDs) - AE/SE - Fetal

Premature closure of ductus arteriosus =...

- pulmonary hypertension

- Tricuspid regurgitation

- Renal failure

Tocolytics - Prostaglandin inhibitors (NSAIDs) - AE/SE - Caution for...

- Platelet disorders (vulnerable to bleeding)

- Renal dysfunction

- NSAID sensitive asthma

- PUD

Tocolytics - Calcium channel blockers - MOA

Blocks voltage gated calcium channel = INHIBITS calcium action on myometrium

Tocolytics - Calcium channel blockers - AE/SE

- Flushing

- Dizziness, headache

- Palpitation

- Reflex tachycardia (hypotension) >> BP down, heart responds by increasing HR to compensate

Glucocorticoid Therapy - Purpose

Speed fetal lung development

Decrease risk of...

- Respiratory distress syndrome

- Brain bleeding

- Necrotizing enterocolitis

- Sepsis

Hormone Therapy - MOA

Application of estrogen/progesterone = +ve effect on bone density

- Also treats menopause