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What is this and when do we use this?
Somatropin is a synthetic GH agonist used in treating GH deficiency in illnesses such as Prader-willi, Turner's, and renal failure. Also it is used in wasting in HIV/AIDS patients.
Describe the actions of GH, direct and indirect effects.
- GH has indirect bone lengthening effect (by acting first of the liver, secreting IGF1, then IGF1 acts on bones). GH also acts directly on adipose tissue (lypolyses).
- Net Effect = Increase blood glucose levels (antagonizes insulin)
- Fun fact (idk if high yield) - Previously GH was obtained by human cadavers, but this would result in Creutzfeldt-jakob disease (CJD)
Adverse effects of GH agonists (somatropin)
- Carpel tunnel syndrome (crushing median nerve by expanding tissue)
- Increase intracranial tension (pseudotumor cerebri)
What is Mecasermin?
Mecasermin is an IGF1 preparation used in cases where GH is not producing a good effect (GH insensitive patients) and for those who have antibodies against GH.
What is the drug that antagonizes GH?
- Pegvisomant - used in acromegaly.
- CAUTION, Check for liver toxicity by checking for increased liver enzymes in blood.
Name the cellular signaling pathway that is involved in Pegvisomant.
Pegvisomant binds (and blocks) GH receptors, inhibiting the JAK-STAT signaling.
What are the dopamine agonists and when do you use them?
- Used for acromegaly. Dopamine blocks prolactin, prolactin and GH have a common lineage. Dopamine agonists may also block GH. It is however the last choice.
What are they?
- The -tropins are Gonado-tropins agonists: FSH and LH
- Urofolli and follitropins are FSH agonists
- Menotropin is both FSH and LH agonist
- hChorionic gonadotropin (hCG can be used for cryptorchidism)
What are the gonadotropin agonists used for?
- Ovulation induction. Many women have anovulation problems that is secondary to hypogonadotropic hypogonadism and polycystic ovary syndrome.
- Inducing ovulation (ovary release of eggs) may be hyperstimulated and the eggs can be secreted into the peritoneum, causing shock which is life threatening. It must be controlled!!!
Explain the protocol of the drugs used for infertility. When (during the cycle) do we use which drugs?
- Some time after ovulation administer hCG. Then retrieve the egg and do in vitro fertilization. Transfer the embryo back into uterus and administer progesterone for support of pregnancy.
- GnRH agonist is used for long term therapy to cut off pituitary and ovarian access during the follicular phase.
- GnRH antagonist is used for short term to cut off pituitary and ovarian access during the follicular phase.
Anti-psychotic drugs fall under which category of drugs?
What are the adverse effects of anti-psychotic drugs?
- Anti-psychotics block dopamine. (help in prolactin production)
- Can cause hyperprolactinoma, leading to galactorrhea and infertility.
- TRH also causes hyperprolactinoma. In hypothyroidism, no T3, T4. No negative feedback, increase TRH, increase prolactin and TSH secretion.
- Are dopamine agonists (D2 receptor agonists (found in the brain))
- Used in acromegaly, hyper-prolactinoma, and parkinson's disease.
What are the adverse affects of taking B-C-ines (bromocriptine, cabergoline)?
- Nausea - dopamine and serotonin are NTs for vomitting.
- postural hypotension
- occasional psychiatric manifestations
- Digital vasospasms.
What is an agonist of oxytocin? (oxytocin is secreted by the posterior pituitary)
- Pitocin (sounds similar (-tocin))
- Used to stimulate uterine contractions at the end of pregnancy, during labor to speed up the process.
- Also contracts myoepithelial cells of the breast.
Adverse effects of oxytocin agonist drug?
- Pitocin can cause seizures and hyponatremia. Oxytocin and ADH both secreted by posterior pituitary. Pitocin looks like ADH. ADH used to retain water. This leads to hyponatremia. Hyponatremia is associated with seizures.
- This is also contraindicated in fetal distress and prematurity. (Check fetal heart rate).
Why can we not take Pitocin early in pregnancy?
Because there are not as many receptors in the myoepithelial cells of the uterus early in pregnancy because estrogen hasn't induced oxytocin receptors yet. Later on, with more estrogen, more receptors, it is possible to speed up labor.
Is an oxytocin antagonist... That's all. Consider this as a treatment for preterm labor.
Pressins and tans
What am I talking bout?
- -pressins are vasopressin receptor agonists (V1 and V2 analogs)
- -tans are vasopressin receptor antagonists
What are the V2 analogs?
- Desmopressin (DDAVP or V2 AVP)
- Used for renal fulid reabsorption. Increases blood volume (reduces urine volume). Increases osmolarity causes release of vasopressin. Desmopressin is more stable and has less effect on blood pressure than vasopressin.
- Terlipressin (or the other -pressin and just remember desmo = V2 (desmo sounds like dos, dos = 2)
- V1 vasoconstricts, which increases blood pressure.
What are the AVP ADH agonists used for?
- Diabetes insipidus
- Nocturnal enuresis
- Mild hemophilia and vWB (it mediates release of factor 8 and vWB)
Vasopressin receptor antagonists?
- the -tans
- Antagonizes both V1 and V2 to treat hyponatremia due to SIADH.
Which drugs used for Diabetes Insipidus?
- Thiazides (non-Li induced DI) - used to induce reflex from the body to increase sodium reabsorption from PCT and reduced GFR
- Amiloride (Li-induced DI)
What does central and nehprogenic DI?
Central means it comes from lack of ADH, just give desmopressin to increase renal fluid retention.
Nephrogenic means there is kidney problems give the other 2, thiazides and amiliorides.