12 - Endocrine Flashcards
- Recombinant GH
- increases release of IGF-1 in liver and cartilage
Somatropin
- given SC
Recombinant IGF-1 agonist
- for children unresponsive to GH therapy
Mecasermin
GH receptor antagonist
- for acromegaly
Pegvisomant
Somastostatin analogue
- suppresses the release of GH, glucagon, insulin, gastrin, IGF-1, serotonin and GI peptides
- octreotide
- lanreotide
FSH analog
- Follitropin Alfa
- Follitropin Beta: recombinant FSH forms
- Menotropin (hMG)
- Urofollitropin: purified preparation from urine of postmenopausal women
LH analog
- Choriogonadotropin Alfa: recombinant hCG
- hCG: given IM
- hMG: mixtures of FSH and LH from postmenopausal womeb
- Lutropin Alfa: recombinant LH
GnRH analog
Leuprolide
- long agonist activity
Other names:
- leuprorelin
- leuprolin
Time of administration of Leuprolide to increase LH and FSH secretion
Intermittent
Time of administration of Leuprolide that reduce LH and FSH secretion
Prolonged and continuous
Remedy for apoplexy and blindness during forst few weeks of therapy (Leuprolide) and temporary exacerbation of precocious puberty or prostate CA
Flutamide
- co-administer
- androgen receptor antagonist
Synthetic human GnRH
Gonadorelin
GnRH antagonist
Ganirelix
- prevent LH surge in controlled ovulation
GnRH antagonist for prostate CA
Degarelix
Dopamine agonist
- inhibits prolactin release
Bromocriptine
SE of bromocriptine
- burning pain and warmth and redness of the extremities
Erythromelalgia
Activates oxytocin receptors
- for labor induction,
- control of postpartum hemorrhage
Oxytocin
Oxytocin receptor blocker
Atosiban
Agonist of peripheral oxytocin receptors
Carbetocin
ADH agonist relatively selective to V2
Desmopressin
ADH Antagonist at V1A and V2 receptors
Conivaptan
This may occur with rapid correction of hyponatremia
Central pontine myelinolysis
ADH antagonist that is more selective for V2
- Tolvaptan
- Lixivaptan
Thyroid drug that has 4:1 ratio of T4:T3
Liotrix
Recombinant human TSH
Thyrotropin
Thyroid drug that has faster onset but shorter half- life
Liothyronine (T3)
Compared to
Levothyroxine (T4)
- inhibits thyroid peroxidase reactions
- blocks iodine organification
- inhibits peripheral conversion of T4 to T3
PTU
- DOC for pregnant
- short FOA
- slow onset of action
- more strongly protein bound
- inhibits thyroid peroxidase
- blocks organification
Methimazole
- DOC for non-pregnant
- prenatal exposure: Aplasia Cutis Congenita
- 10x more potent
- slower excretion
Mainstay of treatment of postpartum hyperthyroidism, in particular during lactation
Methimazole
Related to choanal and esophageal atresia
Methimazole
Emits beta rays causing destruction of thyroid parenchyma
RAI 131I
- preferred for nost patients
- C/I: pregnant or nursing mothers
Patients shoulf be euthyroid or on BB before RAI
Onset of action of RAI
6-12 weeks
Max effect seen of RAI
3-6 months
Thyroid CA associated with radiation exposure
Papillary thyroid CA
- Inhibits iodine organification and hormone release
- reduce size and vascularity of thyroid gland
Potassium iodide
- Lugol’s solution/KISS
Acts through inhibition of thyroglobulin proteolysis
Potassium Iodide
- should not be used alone
- prevents radiation-infuced thyroid damage
Ingestion of iodine causes HYPOTHYROIDISM
Wolf-Chaikpff effect
Ingestion of iodine cause HYPERTHYROIDISM
Jod-Basedow
- seen in thyroid-deficient
- inhibits peripheral conversion of T4 to T3
- control HR and other cardiac abnormalities
- slows pacemaker activity
Propanolol
May be used to treat thyrotoxicosis-related arrhythmias
Emsolol
Drugs inhibit peripheral conversion of T4 to T3
- PTU
- Propanolol
- Htdrocortisone
Controls severe cardiovascular manifestations of Thyroid storm
Propanolol
Protects against shock and also blocks peripheral conversion of T4 to T3
Hydrocortisone
Drug-induced hyperthyroidism
CAM
- Clofibrate
- Amiodarone
- Methadone
Block uptake of iodide by the gland through competitive inhibition of iodide transport mechanism
- perchlorate
- pertechnetate
- thiocyanate
Prototype glucocorticoid
Hydrocortisone (cortisol)
Glucocorticoid with highest anti-inflammatory potency
Betamethasone
Mineralocorticoid with highest salt-retaining potency
Fludrocortisone
Active metabolite of prednisone
Prednisolone
Term used for behavioral changes secondary to steroid use
Steroid rage
Postcoital contraceptive used for emergency contraception (within 72°)
Levonorgestrel
- activates estrogen and/or progesterone receptors
- thickens cervical mucus
- inhibits ovulation
Estrogen ANTAGONIST in breast and CNS
Estrogen AGONIST in urerus, liver and bone
Tamoxifen
Used for hormone-responsive breast CA, prophylaxis of breast CA
Tamoxifen
Full estrogen receptor ANTAGONIST
No agonist effect
Fulvestrant
Given for breast CA patients who are ER/PR (+)
Tamoxifen/toremifene
Estrogen ANTAGONIST in breast, CNS, uterus
AGONIST in liver and bone
Raloxifene
Used for osteoporosis and breast cancer prevention
Raloxifene
- preferred in patient with history of breast CA in the management of hot flushes
Partial agonist of estrogen receptors in pituitary.
Reduces negative feedback by estradiol
Increase FSH and LH output
Clomiphene
Used for induction of ovulation for those who want to get pregnant
Clomiphene
Estrogen synthesis inhibitor by inhibiting aromatase
Anastrazole
- for breast CA and precocious puberty
Irreversible inhibitor of aromatase (testosterone to estradiol)
Exemestane
Ovarian inhibitor (antiandrogen)
- weak cytochrome P450 inhibitor
- partial agonist of progestin and androgen receptors
Danazol
For:
- endometriosis
- fibrocystic disease
- hemophilis
- angioneurotic edema
C/I: pregnancy and breastfeeding
May also act on glucocorticoid receptors
Glucocorticoid synthesis inhibitor
- inhibits desmolase
Aminoglutethimide
For:
- breast CA
- Cushing syndrome
Selective inhibitor of 11 hydroxylation interfering with cortisol anf corticosterone synthesis
Metyrapone
DOC for pregnant wit Cushing syndrome
Metyrapone
Glucocorticoid receptor antagonist
Progesterone receptor antagonist
Mifepristone
Anabolic steroid androgen
- illegal performance enhancement drug in athletes
Oxandrolone
Competitive antagonist at androgen receptor
- for prostate CA
Flutamide
- Antagonist at androgen receptor
- marked progestational effect that suppresses the feedback enhancement of LH and FSH
Cyproterone
For
- hirsutism
- decreases sexual drive in men
Androgen synthesis inhibitor that inhibits 5 alpha-reductase (testosterone to dihydrotestosterone)
Finasteride/Dutasteride
For
- BPH
- male pattern baldness
- hirsutism
Rapid acting Insulin
LAG
- lispro
- aspart
- glulisine
Long acting insulin
- Glargine
- Lantus
- Detemir
Early morning hyperglycemia
3AM: hypoglycemia
7AM: hyperglycemia
Somogyi effect
Treatment for Somogyi effect
Decrease evening insulin
SOMOGYI = SUMOBRA
Early morning hyperglycemia
3AM: normal
7AM: hyperglycemia
Dawn phenomenon
Treatment for Dawn phenomenon
Increase evening insulin
Early morning hyperglycemia
3AM: hyperglycemia
7AM: hyperglycemia
Waning of Insulin Dose
Treatment for waning of insulin dose
Increase evening insulin
Early morning hyperglycemia
3AM: hyperglycemia
7AM: more hyperglycemia
Dawn + Waning
Increase insulin dose
Perior in T1 DM when exogenous insulin requirements decrease due to an increase in endogenous production of insulin
Honeymoon period
Antidiabetic drugs which causes weight gain
GITS
- glinides (non-sulfonylurea insulin secretagogues)
- insulin
- TZD
- SUR
Antidiabetic agents which accelerates gastric emptying time
- GLP 1 agonist
- DPP4 inhibitor
- pramlintide
SUR that has the longest duration of action and disulfiram reaction
Chlorpropramide - 1st gen SUR
Disulfiram drugs
Clara took the Pre-Medical Test in the PM
- chlorpropramide
- cefoperazone
- cefomandole
- cefotetan
- procarbazine
- metronidazole
MOA of SUR
Increase insulin secretion by closing ATP-sensitive K channels
2nd gen SUR which has SE of cholestatic jaundice
Glibenclamide
- most notorious among 2nd gen SUR
1st gen SUR which are highly protein bound
- compete wfor protein binding and may enhance hypoglycemic effects
Tolbutamide
Chlorpropamide
Antidiabetic agents which mag cause hypoglycemia
- insulin
- SUR
- glinides (less)
MOA of glinides
- repaglinide
- nateglinide
- mitiglinide
- Increase insulin secretion by closing ATP-sensitive K channels
- reduces circulating glucose
- increases glycogen, fat and protein formation and gene regulation
Glinide that has the least incidence of hypoglycemia and may be used in CKD patients
Nateglinide
Has the lowest risk of developing hypoglycemia since they have a short duration of action
GLINIDES
Other drugs that cause hypoglycemia
- insulin
- SUR