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What drugs are available to treat pituitary dwarfism?
Somatropin (a group of drugs) and Mecasermin
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What kind of drug is Mecasermin?
Recombinant IGF-1
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What are the adverse effects of Somatropin?
- Hyperglycemia
- High SBP
- interacts w/ glucocorticoids
- Neutralizing antibodies
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What are the adverse effects of Mecasermin?
- Hypoglycemia
- Allergic reactions
- Hypertrophy or tonsils
- Overgrowth of fat, kidneys and facial bones
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Would you use Mecasermin or Somatropin if a patient has non-functional GH receptors?
Mecasermin (IGF-1 analog)
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Would you use Mecasermin or Somatropin if a patient has functioning GH receptors, but low GH levels?
Somatropin
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At what point in a childs growth would it not be useful to give Somatropin?
After epiphysis have closed
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Why can you develop allergic reactions to Mescarmin?
It is a protein
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What drugs should you not give with Somatropins and why?
Glucocorticoids, reverse the effects of GH
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Why do neutralizing antibodies develop against Somatropin?
If person is making some GH themselves, they may develop antibodies against the “invading” ones being given
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What group of drugs would you use to treat acromegaly/gigantism?
Somatostatin analogs or GH receptor antagonists
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What are the somatostatin analogs?
- Octreotide (Sandostatin)
- Lanreotide
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What are the GH receptor antanogists?
Pegvisomant
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By what mechanism do Somatostatin analogs like octrotide and lanreotide act?
- Work through Somatostatin receptor ligands (SRLs)
- Operate similarly to Somatostatin Growth hormone inhibiting release hormone
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Why do Somatostatin analogs (Octreotide and Lanreotide) cause GI side effects?
b/c there are somatostatin receptors in our stomach
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What mechanisms cause Somatostatin analogs (Octreotide and Lanreotide) to have injection site reactions?
- They are a protein
- They prevent lipolysis, so can create fatty acid deposits
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GH receptor antagonists like Pegvisomant are similar to what naturally occurring hormone?
GH
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What rugs should you not give with GH receptor antagonists like Pegvisomant?
Opioids, reason unknown, but they reduce Pegvisomont’s effects
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What are the side effects for GH receptor antagonists like Pegvisomant?
- GI issues
- Injection site reactions
- Abdominal pain
- Gallstones
- Hypo- or hyperglycemia
- Bradycardia (lanreotide)
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What are the side effects for Somatostatin analogs (Octreotide and Lanreotide)?
- GI issues
- lipohypertrophy at injection site reactions
- opioid analgesic interaction
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What drugs can increase DA or stimulate the DA receptor in the anterior pituitary, causing a decrease in prolactin?
- L-DOPA
- Bromocriptine
- Cabergoline
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What drugs can decrease DA or inhibit the DA receptor in the anterior pituitary, causing as increase in prolactin?
- Reserpine
- Antipsychotics
- Alpha-methyl dopa
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What types drugs can be used to treat hyperprolactinemia?
- Dopaimine agonists:
- Ergot-alkaloids from plants
- Non-ergot derived
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What drugs are Ergot-alkaloids from plants, increase DA release and treat hyperprolactinemia?
Cabergoline (D2) and Bromocriptine (D2 and D1)
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Why is Cabergoline preferred over Bromocriptine for treatment of hyperprolactinemia?
- It is more selective: Cabergoline (D2) and Bromocriptine (D2 and D1)
- So, it has less side effects
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What is the MOA of Hyperprolactinemia drugs?
Bind D2 receptors
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What are the side effects of Hyperprolactinemia drugs?
N/V, HA, Dizziness, Personality changes, HYPOtension
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Side effects for Cabergoline (D2) and Bromocriptine (D2 and D1) are caused by what Characteristics?
Binding to sites other than D2: such as D1 (bromocriptine), adrenergic and seratonergic receptors
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Vasopressin is released from where?
Posterior Pituitary
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What are the vasopressin agonists?
8-L-arginine vasopressin (Pitressin), Desmopressin and Telipressin
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Which Vasopressin agonist is V1A selective?
8-L-arginine vasopressin (Pitressin) and Telipressin
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Which Vasopressin agonist is V2 selective?
Desmopressin
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What are the routes of administration for Desmopressin?
SQ, IV, Intranasal and Oral
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What are the routes of administration for 8-L-arginine?
IM, SQ, Intranasal
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What is the difference between 8-L-arginine vasopressin and terlipressin?
Terlipressin is a synthetic analog with a longer t1/2
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What are the vasopressin antagonists called as a group?
Vaptans
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What are the Vaptans/Vasopressin antagonists?
Conivaptan and Tolvaptan
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Which vaptan/vasopressin antagonist is selective for V1A and V2 receptors?
Conivaptan
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Which vaptan/vasopressin antagonist is V2 selective?
Tolvaptan
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What are the indications for 8-arginine vasopressin (at the V1A receptor)?
- Postoperative ileus and abdominal distension
- Reduce/stop bleeding from esophageal varicies
- Reduce general bleeding
- Diabetes insipidus
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What are the indications of Desmopresin (at the V2 receptors)?
- Central Diabetes insipidus
- Type 1 von willebrand’s disease
- Nocturnal enuresis
- Post lumbar puncture headache
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What are the adverse effects of vasopressin drugs?
- Nausea
- HA
- Abdominal cramps
- Allergic reactions
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Would you give a vaptan for Hyponatremia?
Yes
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What is the route of administration when giving conivaptan for Hyponatremia?
IV
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What is the route of administration when giving tolvaptan for Hyponatremia?
PO
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What is the MOA of Oxytocin?
- Sustained uterine contractions by acting on receptors linked to Gq/11 and Gi
- Contracts myoepithelial cells surrounding acinar cells in the breast leading to milk ejection
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What are the indications for Oxytocin?
- Induce labor (IV)
- In utero circulation test (IV)
- Overcome breast engorgement (Intranasal)
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What are the adverse effects of Oxytocin?
HTN, uterine rupture and fetal death
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Where is Oxytocin released from?
Posterior pituitary
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