DRUGS AFFECTING HYPOTALMIC, PITUITARY, and THYROID FUNCTION Flashcards
Somatropin
MOA
INDICATION
Somatropin
MOA
hGH (human growth hormone) that acts through GH receptors to increase the production of IGF-1
INDICATION
Kids under 2 years old benefit the most from hGH therapy
Adults get increased muscle mass and decreased adipose tissue
HIV associated wasting
Somatotropin Side Effects (children, adults)
Somatropin
SIDE EFFECTS
Children:
Few typically; intracranial HTN, papilledema, visual changes, headache, N/V
LEUKEMIA – reported in kids 1-2 yrs out from tx for pediatric tumors
Adults:
• peripheral edema, carpal tunnel syndrome, arthralgia, myalgia
Mescasermin
MOA
Indication
Mecasermin
MOA
hIGF-1 complexed with hIGF binding protein 3 (binding protein increases half-life)
INDICATION
IGF-1 deficiency in children (kids don’t respond to growth hormone)
Mescamerimin
Side Effects
Mecasermin
SIDE EFFECTS:
Hypoglycemia, intracranial HTN, increased liver enzymes
Pegvisomant
MOA
Indications
Pegvisomant
MOA
Growth hormone receptor antagonist, decreases levels of IGF-1; PEG added to increase duration of action
INDICATION
Acromegaly
Pegvisomant
Side Effects
Pegvisomant
SIDE EFFECTS
Increased Liver enzymes
What is the general indication for Somatotropin and Mescamerimin?
Natural Hormones and associated drugs: Somatropin, Mecasermin
GH analogs are used in adults who have general obesity, low muscle mass, and reduced cardiac output from decreased GH. It can also decrease mortality from CV disease and AIDS associated wasting
Octreotide
Administration
MOA
Octreotide/Lantreotide
Administration
Octreotide: 3x per day injections
Lantreotide: 1 injection every 4 weeks
MOA
Somatostain analog
Octreotide
Indications
Side Effects
Octreotide/Lantreotide
INDICATION
Acromegaly; Inoperable pituitary tumors
SIDE EFFECTS
Diarrhea, nausea, abdominal pain
Lantreotide
Administration
MOA
Octreotide/Lantreotide
Administration
Octreotide: 3x per day injections
Lantreotide: 1 injection every 4 weeks
MOA
Somatostain analog
Lantreotide
Indication
Side Effects
Octreotide/Lantreotide
INDICATION
Acromegaly; Inoperable pituitary tumors
SIDE EFFECTS
Diarrhea, nausea, abdominal pain
What is the general indication for growth hormone inhibitors?
• name them.
GH inhibitors: Octreotide/Lantreotide, Pegvisomant
Somatostatin is a negative regulator or GH and TSH. Analogs of somatostatin are the best treatment when pituitary surgery is impossible.
What drugs inhibit Prolactin secretion?
• indication?
Drugs inhibiting Prolactin Secretion: Carbergoline, Bromocriptine
Indication:
• these drugs are recommended BEFORE surgical intervention in prolactinomas (this is different than GH tumors)
Cabergoline
MOA
Inhdication
Cabergoline/Bromocriptine
MOA
Cabergoline: High affinity for D2 receptors
Bromocriptine: Dopamine receptor Agonist (not well tolerated)
INDICATION
Used in the treatment of hyperprolactinemia associated with pituitary ademomas
Cabergoline
Side Effects
Cabergoline/Bromocriptine
SIDE EFFECTS
GI disturbances, orthostatic hypoTN, HA, psychiatric disturbances, pulmonary infiltrates
Bromocriptine
MOA
Indication
Cabergoline/Bromocriptine
MOA
Cabergoline: High affinity for D2 receptors
Bromocriptine: Dopamine receptor Agonist (not well tolerated)
INDICATION
Used in the treatment of hyperprolactinemia associated with pituitary ademomas
Bromocriptine
Side Effects
Cabergoline/Bromocriptine
SIDE EFFECTS
GI disturbances, orthostatic hypoTN, HA, psychiatric disturbances, pulmonary infiltrates
Protirelin
MOA
Indication
Protirelin
MOA
TRH that stimulates TSH release from pituitary
INDICATION
Used in thyroid function testing
Thyrotropin
Thyrotropin (TSH)
MOA
TSH
INDICATION
Used in diagnostics for thyroglobulin levels
Levothyroxine
MOA
Indication
Levothyroxine, Liothyronine Sodium, Liotrix
Administration
MOA
Levothryoxine: L-T4 – may take longer to reach steady state
Liothyronine Sodium: L-T3
Liotrix: Mixture of T4 and T3
INDICATION
Hypothyroidism
Liothyronine Sodium
MOA
Indication
Levothyroxine, Liothyronine Sodium, Liotrix
Administration
MOA
Levothryoxine: L-T4 – may take longer to reach steady state
Liothyronine Sodium: L-T3
Liotrix: Mixture of T4 and T3
INDICATION
Hypothyroidism
Liotrix
MOA
Indication
Levothyroxine, Liothyronine Sodium, Liotrix
Administration
MOA
Levothryoxine: L-T4 – may take longer to reach steady state
Liothyronine Sodium: L-T3
Liotrix: Mixture of T4 and T3
INDICATION
Hypothyroidism
Name the thyroid hormone analogs and their side effects.
Levothyroxine, Liothyronine Sodium, Liotrix
SIDE EFFECTS
Hyperthyroidism (Tachycardia, cardiac hypertrophy, Heat Intolerantce, decreased PVR, increased pulse pressure)
What should you keep in mind when administering thyroid replacement therapy?
• how does administration differ in children?
Thyroid Hormone Replacement Therapies: Levothyroxine, liothyronine sodium, liotrix
NOTE: These may have to be administered in higher doses to children and it may take several weeks to reach a steady state level (b/c it take 4-5 half-lives to reach the steady state level of a drug and T3 and T4 have 24 hour and 4 day half-lives)
Name the 3 anti-thyroid drugs.
Anti-thyroid Drugs (THIOAMIDES): PTU (propylthiouracil), methimazole, carbimazole
PTU (propylthiouricil)
Administration
MOA
PTU (propylthiouracil)
Administration
Shorter half-life than methimazole and less potent
MOA
Inhibition of thyroid peroxidase (iodination and coupling) and inhibits peripheral conversion of T4 to T3 (via 5’-iodinase)
PTU (propylthiouricil)
Indication
Side Effects
PTU (propylthiouracil)
INDICATION
Hyperthyroidism; Safer for pregnant women because it does NOT cross the placenta and is not excreted in milk
SIDE EFFECTS
Agranulocytosis, Skin rash, HypOthyroidism
Methimazole/Carbimazole
Administration
MOA
Indication
Methimazole/Carbimazole
Administration
Longer half-life than PTU
MOA
Inhibition of thyroid peroxidase catalyzed iodination and coupling
INDICATION
Hyperthyroidism
Methimazole/Carbimazole
Side Effects
Contraindications
Methimazole/Carbimazole
SIDE EFFECTS
Agranulocytosis, Skin rash, Hypothyroidism; can cross the placenta to cause fetal hypothyroidism
CONTRAINDICATIONS
DO NOT GIVE TO WOMEN THAT ARE PREGNANT OR NURSING
What endocrine risk is associated with administering iodine contrast media?
Iodinate Contrast media: can cause hyperthyroidism in euthyroid patients or thyroid storm in hyperthyroid patients
Iodine/Lugol’s Solution
MOA
Indication
Iodine/ Lugol’s Solution
MOA
High doses work to inhibit thyroid peroxidase and prevent thyroid hormone synthesis at all levels in the thyroid (Wolff-Chaikoff effect). Works only in SHORT TERM Tx.
INDICATION
- *Thyroid Storm**
- Pre-operative tx for thyroid – decreases vascularity fragility and size of hyperplastic thyroids before surgery*
Lugol’s Solution/Iodine
Side Effects
Contraindications
Iodine/ Lugol’s Solution
SIDE EFFECTS
Rare toxicity – Rash, drug fever, metallic taste, bleeding disorders, anaphylaxis
CONTRAINDICATIONS
DO NOT use prior to radioactive iodine tx (makes radioactive iodide less effective)
Radioactive Iodine
MOA
Indication
Radioactive Iodine
MOA
Concentrates in the thyroid where beta radiation will destroy all/part of the parenchymal cells, tissue surrounding thyroid is left alone
INDICATION
Hyperthyroidism
Radioactive Iodine
Contraindications
Radioactive Iodine
CONTRAINDICATIONS
People must be 35 or older; NOT in women of child-bearing age