BLOCK 3 PMY 302 - DRUGS to KNOW
Q&A
Somatropin Drug Class Synthetic recombinant human growth hormone
Somatropin MOA Identical in action and abilities like endogenous secreted GH (stimulating
proliferation of bone growth plates and increased linear bone growth, promotion of protein synthesis
throughout the body)
Somatropin/Somatrem dosing Daily dosing dependent and adjusted to individual clinical response
and IGF-1 levels
Somatropin/Somatrem pharmacokinetics Following SC injection, 80% of the drug will be
systemically available
Somatropin/somatrem results and monitoring Response to GH therapy is measured every 3-6
months by height and bone age determinations
Somatropin/Somatrem Therapeutic use Childhood Dwarfism/Growth hormone deficiency
disorders
Somatrem Drug class Analog of GH; synthetic recombinant human growth hormone with Extra
amino acid noted in protein makeup
Somatrem MOA Similar to somatropin
Octreotide Acetate and Lanreotide drug class synthetic analogs of somatostatin
Octreotide Acetate and Lanreotide MOA acts identical to somatostatin to directly inhibit GH
release from the anterior pituitary which effectively decreases circulating GH and IGF-1 levels
,Octreotide Acetate and Lanreotide Dosing Long-acting depots allow for once-a-month IM dosing
due to gradual release formula (10-20 mg/4 weeks) T ½: 1-2 hours
Octreotide Acetate and Lanreotide Therapeutic effects suppresses GH hypersecretions, reduces
pituitary adenoma overgrowth, and normalizing levels of GH and IGF-1
Octreotide acetate/Lanreotide/Pegvisomant Use Acromegaly/Gigantism Tx
Pegvisomant Drug class GH receptor antagonist
Pegvisomant MOA Blocks actions of GH and reduces the levels of circulating IGF-1
Pegvisomant Dosing daily SubQ injections; increases dose until serum IGF-1 levels are maintained
to be within the age-appropriate/normal range (usually within 12 months, pt. Will have normal or next
to normal levels of IGF-1)
Pegvisomant drug structure Extremely similar protein structure to GH but acts as a receptor
antagonist
Bromocriptine/Cabergoline drug class Dopamine Receptor Agonists
Bromocriptine/Cabergoline MOA Decreases prolactin production and secretions by prolactin-
secreting pituitary tumors; mimics the actions of dopamine and causes inhibition of prolactin secretion
Bromocriptine/Cabergoline Pharmacokinetics Orally Active and effective use in 80-85% of cases
Bromocriptine/Cabergoline Therapeutic effects Reduces tumor size, suppresses galactorrhea and
restores normal ovulatory menstrual cycles
,Bromocriptine special consideration Longer track record of safety in use and cheaper to produce
(DOC/more commonly used)
Cabergoline special consideration Has higher reported affinity for D2 receptors
Desmopressin Drug Class DDAVP/Vasopressin synthetic analog
Desmopressin MOA activates V2 receptors in the kidney's collecting ducts, reabsorbing water into
plasma and concentrating the urine (prevents water from leaving the body)
Desmopressin compared to ADH Longer noted serum T ½ compared to ADH (DDAVP t ½ = 75 min)
(ADH t ½ = >10 min)
Desmopressin Structure Almost identical to ADH except for D-Amino acid in chemical chain
sequence (ADH has L-Amino Acid) *NOTE: Has a greater selectivity for V2 receptors compared to typical
ADH*
Desmopressin Pharmacokinetics Extremely potent drug; Tablet (0.1-0.2 mg) or nasal spray
(0.01mg)
Desmopressin Outcomes of DI Excessive urine production controlled with 0.1mg/3x daily
Desmopressin Outcomes of Nocturnal Enuresis 4 months of Tx (0.2-0.4mg/daily) will decrease
average wet nights from 10/week to 6-7/2 weeks
Pitocin Drug class Synthetic Oxytocin
Pitocin MOA Stimulates uterine contractions during labor to strength (typically used in
induction/emergency scenarios if birth is taking an extremely long time)
Pitocin Pharmacokinetics Given IV at low doses; used in OB/GYN practice
, Hydrocortisone Drug class glucocorticoid replacement therapy
Hydrocortisone MOA mimics actions of cortisol (increasing gluconeogenesis, protein, and lipid
catabolism and body resistance response to stress)
Hydrocortisone Use replacement therapies for both adrenal insufficiencies and anti-
inflammatory/immunosuppressive treatments (Glucocorticoid of choice in replacement tx since adverse
effects are minimized)
Hydrocortisone Pharmacokinetics Short-acting drug ( t ½ 80 min that requires 2-3 doses/daily);
The highest dose is an admin in the morning and smaller doses are given in the evening to mimic natural
cortisol blood levels // Short-acting preps are preferred because they can be adjusted readily to reduce
adverse effects and Extra doses can be given for bodily stresses (infections, fever, injury)
Fludrocortisone Drug class mineralocorticoid replacement therapy
Fludrocortisone MOA mimics actions of aldosterone (salt retention and elimination of K+; raises
BP)
Fludrocortisone Use Provides mineralocorticoid activity in replacement therapies for adrenal
insufficiencies
Fludrocortisone Pharmacokinetics T ½ 18-36 hours (long-lasting) daily dose; dosing is tailored to
manage BP and fluid balances
Prednisone drug class glucocorticoid replacement therapy
Prednisone MOA mimics actions of cortisol (increasing gluconeogenesis, protein, and lipid
catabolism, and body resistance response to stress) and has high anti-inflammatory properties; low
doses and short term use is important to prevent HPA axis suppression
Q&A
Somatropin Drug Class Synthetic recombinant human growth hormone
Somatropin MOA Identical in action and abilities like endogenous secreted GH (stimulating
proliferation of bone growth plates and increased linear bone growth, promotion of protein synthesis
throughout the body)
Somatropin/Somatrem dosing Daily dosing dependent and adjusted to individual clinical response
and IGF-1 levels
Somatropin/Somatrem pharmacokinetics Following SC injection, 80% of the drug will be
systemically available
Somatropin/somatrem results and monitoring Response to GH therapy is measured every 3-6
months by height and bone age determinations
Somatropin/Somatrem Therapeutic use Childhood Dwarfism/Growth hormone deficiency
disorders
Somatrem Drug class Analog of GH; synthetic recombinant human growth hormone with Extra
amino acid noted in protein makeup
Somatrem MOA Similar to somatropin
Octreotide Acetate and Lanreotide drug class synthetic analogs of somatostatin
Octreotide Acetate and Lanreotide MOA acts identical to somatostatin to directly inhibit GH
release from the anterior pituitary which effectively decreases circulating GH and IGF-1 levels
,Octreotide Acetate and Lanreotide Dosing Long-acting depots allow for once-a-month IM dosing
due to gradual release formula (10-20 mg/4 weeks) T ½: 1-2 hours
Octreotide Acetate and Lanreotide Therapeutic effects suppresses GH hypersecretions, reduces
pituitary adenoma overgrowth, and normalizing levels of GH and IGF-1
Octreotide acetate/Lanreotide/Pegvisomant Use Acromegaly/Gigantism Tx
Pegvisomant Drug class GH receptor antagonist
Pegvisomant MOA Blocks actions of GH and reduces the levels of circulating IGF-1
Pegvisomant Dosing daily SubQ injections; increases dose until serum IGF-1 levels are maintained
to be within the age-appropriate/normal range (usually within 12 months, pt. Will have normal or next
to normal levels of IGF-1)
Pegvisomant drug structure Extremely similar protein structure to GH but acts as a receptor
antagonist
Bromocriptine/Cabergoline drug class Dopamine Receptor Agonists
Bromocriptine/Cabergoline MOA Decreases prolactin production and secretions by prolactin-
secreting pituitary tumors; mimics the actions of dopamine and causes inhibition of prolactin secretion
Bromocriptine/Cabergoline Pharmacokinetics Orally Active and effective use in 80-85% of cases
Bromocriptine/Cabergoline Therapeutic effects Reduces tumor size, suppresses galactorrhea and
restores normal ovulatory menstrual cycles
,Bromocriptine special consideration Longer track record of safety in use and cheaper to produce
(DOC/more commonly used)
Cabergoline special consideration Has higher reported affinity for D2 receptors
Desmopressin Drug Class DDAVP/Vasopressin synthetic analog
Desmopressin MOA activates V2 receptors in the kidney's collecting ducts, reabsorbing water into
plasma and concentrating the urine (prevents water from leaving the body)
Desmopressin compared to ADH Longer noted serum T ½ compared to ADH (DDAVP t ½ = 75 min)
(ADH t ½ = >10 min)
Desmopressin Structure Almost identical to ADH except for D-Amino acid in chemical chain
sequence (ADH has L-Amino Acid) *NOTE: Has a greater selectivity for V2 receptors compared to typical
ADH*
Desmopressin Pharmacokinetics Extremely potent drug; Tablet (0.1-0.2 mg) or nasal spray
(0.01mg)
Desmopressin Outcomes of DI Excessive urine production controlled with 0.1mg/3x daily
Desmopressin Outcomes of Nocturnal Enuresis 4 months of Tx (0.2-0.4mg/daily) will decrease
average wet nights from 10/week to 6-7/2 weeks
Pitocin Drug class Synthetic Oxytocin
Pitocin MOA Stimulates uterine contractions during labor to strength (typically used in
induction/emergency scenarios if birth is taking an extremely long time)
Pitocin Pharmacokinetics Given IV at low doses; used in OB/GYN practice
, Hydrocortisone Drug class glucocorticoid replacement therapy
Hydrocortisone MOA mimics actions of cortisol (increasing gluconeogenesis, protein, and lipid
catabolism and body resistance response to stress)
Hydrocortisone Use replacement therapies for both adrenal insufficiencies and anti-
inflammatory/immunosuppressive treatments (Glucocorticoid of choice in replacement tx since adverse
effects are minimized)
Hydrocortisone Pharmacokinetics Short-acting drug ( t ½ 80 min that requires 2-3 doses/daily);
The highest dose is an admin in the morning and smaller doses are given in the evening to mimic natural
cortisol blood levels // Short-acting preps are preferred because they can be adjusted readily to reduce
adverse effects and Extra doses can be given for bodily stresses (infections, fever, injury)
Fludrocortisone Drug class mineralocorticoid replacement therapy
Fludrocortisone MOA mimics actions of aldosterone (salt retention and elimination of K+; raises
BP)
Fludrocortisone Use Provides mineralocorticoid activity in replacement therapies for adrenal
insufficiencies
Fludrocortisone Pharmacokinetics T ½ 18-36 hours (long-lasting) daily dose; dosing is tailored to
manage BP and fluid balances
Prednisone drug class glucocorticoid replacement therapy
Prednisone MOA mimics actions of cortisol (increasing gluconeogenesis, protein, and lipid
catabolism, and body resistance response to stress) and has high anti-inflammatory properties; low
doses and short term use is important to prevent HPA axis suppression
