Drugs list 3 Flashcards
Ganirelix
Drug class:
- Ganirelix is a synthetic decapeptide
- competitive gonadotropin-releasing hormone (GnRH) antagonist.
Indication:
- down regulation (suppression) of the pituitary in order to prevent premature ovulation whilst an IVF cycle so that physician can remove eggs directly from the ovaries.
- typically woman has 4-6 days of ganirelix before egg retrieval
- given as injection subcutaneous
Derived from endogenous GnRH, ganirelix has amino acid substitutions. Ganirelix is indicated for controlled ovarian hyperstimulation in assisted reproduction techniques
- Ganirelix injection is used as a fertility medicine to prevent premature luteinizing hormone (LH) surges or ovulation in women undergoing fertility treatment of controlled ovarian hyperstimulation
rFSH
- Human recombinant follicle stimulating hormone
- example of one is Follitropin
Indication:
- used in IVF to stimulate ovaries. Usually used in combination with GnRH
- used to stimulate follicle development in women
- women who and men who have hypogonadism to stimulate follicles in IVF (fertility) or ovulation.
- In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis
Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF).
rFSH mechanism of action
-Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH).
-FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor.
-Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway
- which is known to regulate many other metabolic and related survival/maturation functions in cells.
Folic acid
Folic acid is a nutrient used to treat megaloblastic anemia and is found in many supplements.
When the baby is developing early during pregnancy, folic acid helps form the neural tube. Folic acid is very important because it can help prevent some major birth defects of the baby’s brain (anencephaly) and spine (spina bifida)
Thalidomide
Indication: Multiple Myeloma
MOA:
- Thalidomide binds to cerebron, a component of the E3 ubiquitin ligase complex to selectively degrade the transcription factor IKZF3 and IKZF1
- These 2 transcription factors vital for the proliferation and survival of malignant myeloma cells.
YOU CANNOT TAKE THALIDOMIDE IF YOU PREGNANT
What is the relationship of Thalidomide with pregnancy
Thalidomide was a widely used drug in the late 1950s and early 1960s for the treatment of nausea in pregnant women. It became apparent in the 1960s that thalidomide treatment resulted in severe birth defects in thousands of children.
Abnormalities of the hands and arms are most commonly seen and include a very specific abnormality termed phocomelia (where the hands are attached close to the body and the arms are absent or under-developed).
Magnesium sulphate
- seizures/convulsions in pregnancy, nephritis in children, magnesium deficiency and tetany (involuntary muscle contractions)
- Magnesium inhibits Ca2+ influx through dihydropyridine-sensitive, voltage-dependent channels. This accounts for much of its relaxant action on vascular smooth muscle.
- Magnesium sulfate reduces striated muscle contractions and blocks peripheral neuromuscular transmission by reducing acetylcholine release at the myoneural junction.
Labetolol
Drug class: alpha and beta adrenergic antagonist
Indication:
- angina
- hypertension
- sympathetic overactivity syndrome
MOA:
- Labetalol non-selectively antagonizes beta-adrenergic receptors, and selectively antagonizes alpha-1-adrenergic receptors.
Antagonism of alpha-1-adrenergic receptors leads to vasodilation and decreased vascular resistance. This leads to a decrease in blood pressure that is most pronounced while standing.
Antagonism of beta-1-adrenergic receptors leads to a slight decrease in heart rate.
Antagonism of beta-2-adrenergic receptors leads to some of the side effects of labetalol such as bronchospasms, however this may be slightly attenuated by alpha-1-adrenergic antagonism.
Labetalol leads to sustained vasodilation over the long term without a significant decrease in cardiac output or stroke volume, and a minimal decrease in heart rate
Methyldopa
Indication: hypertension alone or in combination with hydrochlorothiazide
MOA: alpha-2 adrenergic agonist
Sodium Valporate
Drug class: anticonvulsant
Indication:
- Control complex partial seizures
- simplex and complex absence seizures
Oxytocin
Drug class: recombinant hormone
Indication:
- Induce or strengthen uterine contractions in pregnant women to aid in labor and delivery or to control postpartum bleeding.
Oxytocin plays a vital role in labour and delivery.9 The hormone is produced in the hypothalamus and is secreted from the paraventricular nucleus to the posterior pituitary where it is stored.9,10 It is then released in pulses during childbirth to induce uterine contractions.9
The concentration of oxytocin receptors on the myometrium increases significantly during pregnancy and reaches a peak in early labor.
Activation of oxytocin receptors on the myometrium triggers a downstream cascade that leads to increased intracellular calcium in uterine myofibrils which strengthens and increases the frequency of uterine contractions.
Flucloxacillin
Drug class:
- penicillin beta lactam antibiotic
Indications: used in the treatment of bacterial infections caused by susceptible, usually gram-positive, organisms
MOA:
- binds to penicillin-binding proteins.
- this inhibits the third and last stage of bacterial wall synthesis
Tetracyline
Gentamycin
Somatotropin aka growth hormone
- Hypothalamus releases Growth hormone releasing hormone ( GHRH) which then goes to the anterior pituitary.
- GNRH causes the release of somatotropin from somatotroph cells.
NEGATIVE FEEDBACK OF GROWTH HORMONE:
Now there are a few negative feedback loops that generally control the release of growth hormone.
First, increased levels of growth-hormone-releasing hormone in the blood signals the hypothalamus to stop making more.
Second, when growth hormone reaches tissues like the liver, muscles, and bones, they make somatomedins, which are hormones that signal the anterior pituitary to stop producing growth hormone.
Third, growth hormone and somatomedins together signal to the hypothalamus to produce somatostatin, which is also called the growth hormone inhibiting hormone.
In the pituitary, it blocks growth hormone releasing hormone from acting on the somatotroph cells, so that secretion of growth hormone is inhibited.
In addition to the hypothalamus, somatostatin is also secreted in the gastrointestinal tract by the delta (δ) cells of the pancreas, where it inhibits the release of other hormones, like insulin, glucagon, and vasoactive intestinal peptides, as well as gastrin, from the stomach and small intestine.
Direct and indirect effects of somatotropin
Growth hormone also has indirect effects, which are seen in certain tissues like the liver, skeletal muscles, bones, and kidneys, where growth hormone stimulates the steady release of a type of somatomedin called somatomedin C, which is also called insulin-like growth factor 1, or IGF-1.
This IGF-1 then binds to insulin-like growth factor 1 receptors as well as insulin receptors, and promotes cellular metabolism, prevents cell death, and increase the rate of cell division and differentiation throughout the body.
In the muscles, it stimulates amino acid uptake into the muscle cells, which helps with protein production and muscle growth. It’s also the key hormone that stimulates the growth in length of long bones.
IGF-1 acts on the epiphyseal cartilage, or growth plates, of the bones, and stimulates the activity of osteoblasts in the bones and chondrocytes in the cartilage. This helps boost growth, particularly during the growth spurts of puberty.
