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What drugs are available to treat pituitary dwarfism?
Somatropin (a group of drugs) and Mecasermin
What kind of drug is Mecasermin?
What are the adverse effects of Somatropin?
- High SBP
- interacts w/ glucocorticoids
- Neutralizing antibodies
What are the adverse effects of Mecasermin?
- Allergic reactions
- Hypertrophy or tonsils
- Overgrowth of fat, kidneys and facial bones
Would you use Mecasermin or Somatropin if a patient has non-functional GH receptors?
Mecasermin (IGF-1 analog)
Would you use Mecasermin or Somatropin if a patient has functioning GH receptors, but low GH levels?
At what point in a childs growth would it not be useful to give Somatropin?
After epiphysis have closed
Why can you develop allergic reactions to Mescarmin?
It is a protein
What drugs should you not give with Somatropins and why?
Glucocorticoids, reverse the effects of GH
Why do neutralizing antibodies develop against Somatropin?
If person is making some GH themselves, they may develop antibodies against the “invading” ones being given
What group of drugs would you use to treat acromegaly/gigantism?
Somatostatin analogs or GH receptor antagonists
What are the somatostatin analogs?
- Octreotide (Sandostatin)
What are the GH receptor antanogists?
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
Why do Somatostatin analogs (Octreotide and Lanreotide) cause GI side effects?
b/c there are somatostatin receptors in our stomach
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
GH receptor antagonists like Pegvisomant are similar to what naturally occurring hormone?
What rugs should you not give with GH receptor antagonists like Pegvisomant?
Opioids, reason unknown, but they reduce Pegvisomont’s effects
What are the side effects for GH receptor antagonists like Pegvisomant?
- GI issues
- Injection site reactions
- Abdominal pain
- Hypo- or hyperglycemia
- Bradycardia (lanreotide)
What are the side effects for Somatostatin analogs (Octreotide and Lanreotide)?
- GI issues
- lipohypertrophy at injection site reactions
- opioid analgesic interaction
What drugs can increase DA or stimulate the DA receptor in the anterior pituitary, causing a decrease in prolactin?
What drugs can decrease DA or inhibit the DA receptor in the anterior pituitary, causing as increase in prolactin?
- Alpha-methyl dopa
What types drugs can be used to treat hyperprolactinemia?
- Dopaimine agonists:
- Ergot-alkaloids from plants
- Non-ergot derived
What drugs are Ergot-alkaloids from plants, increase DA release and treat hyperprolactinemia?
Cabergoline (D2) and Bromocriptine (D2 and D1)
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
What is the MOA of Hyperprolactinemia drugs?
Bind D2 receptors
What are the side effects of Hyperprolactinemia drugs?
N/V, HA, Dizziness, Personality changes, HYPOtension
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
Vasopressin is released from where?
What are the vasopressin agonists?
8-L-arginine vasopressin (Pitressin), Desmopressin and Telipressin
Which Vasopressin agonist is V1A selective?
8-L-arginine vasopressin (Pitressin) and Telipressin
Which Vasopressin agonist is V2 selective?
What are the routes of administration for Desmopressin?
SQ, IV, Intranasal and Oral
What are the routes of administration for 8-L-arginine?
IM, SQ, Intranasal
What is the difference between 8-L-arginine vasopressin and terlipressin?
Terlipressin is a synthetic analog with a longer t1/2
What are the vasopressin antagonists called as a group?
What are the Vaptans/Vasopressin antagonists?
Conivaptan and Tolvaptan
Which vaptan/vasopressin antagonist is selective for V1A and V2 receptors?
Which vaptan/vasopressin antagonist is V2 selective?
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
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
What are the adverse effects of vasopressin drugs?
- Abdominal cramps
- Allergic reactions
Would you give a vaptan for Hyponatremia?
What is the route of administration when giving conivaptan for Hyponatremia?
What is the route of administration when giving tolvaptan for Hyponatremia?
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
What are the indications for Oxytocin?
- Induce labor (IV)
- In utero circulation test (IV)
- Overcome breast engorgement (Intranasal)
What are the adverse effects of Oxytocin?
HTN, uterine rupture and fetal death
Where is Oxytocin released from?