Term
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Definition
Drug of choice for replacement therapy
Has equal activity at glucocorticoid and mineralocorticoid receptors
Short DOA |
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Term
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Definition
Bisphosphonate
Cross between 2nd and 3rd generation
aminoalkyl side chain at C1 increases anti-resorptive potency 10-fold (2nd gen) but has 3rd gen potency |
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Term
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Definition
Bisphosphonate
Third Generation- Incorporation of a nitrogen heterocycle at C1 further enhances anti-resorptive potency |
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Term
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Definition
Bisphosphonate
2nd Generation- Incorporation of an aminoalkyl side chain at C1 increases anti-resorptive potency 10-fold, allows for separation between antiresorptive and bone mineralization effects |
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Term
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Definition
Bisphosphonate
2nd generation- has aminoalkyl chain at C1 |
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Term
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Definition
Bisphosphonate
1st generation
Generally not used because also inhibits bone mineralization |
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Term
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Definition
Bisphosphonate
1st generation
Generally not used because also inhibits bone mineralization |
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Term
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Definition
Osteoporosis Treatment
MOA: similar to PTH; stimulates osteoblast function, increases gastrointestinal calcium absorption, and increases renal tubular reabsorption of calcium. Treatment with teriparatide results in increased bone mineral density and bone mass.
Drawbacks: very expensive and has been linked to osteosarcoma (bone cancer) |
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Term
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Definition
Given as oral solution in one dose; must collect urine and feces for 48 hours because it is radioactive. Want dose that makes patient euthyroid, not kill all thyroid
After 10 years ~30% of patients become hypothyroid |
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Term
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Definition
Thiourea
Mechanism of Action of Thioureas
↓ thyroid peroxidase reactions
↓ iodine organification
↓ coupling of iodotyrosines (MITS & DITS)
↔ iodide uptake |
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Term
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Definition
Thiourea-- prodrug of Methimazole
Mechanism of Action of Thioureas
↓ thyroid peroxidase reactions
↓ iodine organification
↓ coupling of iodotyrosines (MITS & DITS)
↔ iodide uptake |
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Term
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Definition
Thiourea
Mechanism of Action of Thioureas
↓ thyroid peroxidase reactions
↓ iodine organification
↓ peripheral deiodination (PTU only)—ability to change T4 to T3
↔ iodide uptake |
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Term
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Definition
100% T4
The body converts T4 to T3 as needed
Metabolism of levothyroxine – increase w/ phenytoin & carbamazepine (requires increased synthroid dose)
Don’t take Levo-thyroxine with – iron, cholestyramine, Sucralfate because they can bind together and levothyroxine won’t be absorbed |
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Term
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Definition
| MOA: Androgen antagonist - it blocks the androgen receptor but also blocks negative feedback so that there is actually an increase in circulating testosterone Must give enough to out-compete testosterone; dose increases with time |
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Term
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Definition
| MOA: Inhibits the enzyme 5-α reductase—enzyme that converts testosterone to dihydrotestosterone (DHT) [prostate responds only to DHT, not regular testosterone] |
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Term
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Definition
BPH Therapy; alpha antagonist
MOA: Blockade of alpha receptors reduces the tone at the bladder neck and urethra enabling urine to flow more freely |
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Term
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Definition
BPH Therapy; alpha antagonist
MOA: Blockade of alpha receptors reduces the tone at the bladder neck and urethra enabling urine to flow more freely |
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Term
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Definition
BPH Therapy; alpha 1a antagonist
MOA: Blockade of alpha receptors reduces the tone at the bladder neck and urethra enabling urine to flow more freely |
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Term
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Definition
MOA: Phosphodiesterase-5 Inhibitors
Inhibit the breakdown of cGMP, which maintains bloodflow/vasodilation to the penis and maintains erection. Will not cause an erection unless man is actually aroused
No evidence that it improves sexual function, although could increase duration
May lead to priapism (abnormally long erection) if abused |
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Term
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Definition
MOA: Phosphodiesterase-5 Inhibitors
Inhibit the breakdown of cGMP, which maintains bloodflow/vasodilation to the penis and maintains erection. Will not cause an erection unless man is actually aroused
No evidence that it improves sexual function, although could increase duration
May lead to priapism (abnormally long erection) if abused |
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Term
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Definition
MOA: Phosphodiesterase-5 Inhibitors
Inhibit the breakdown of cGMP, which maintains bloodflow/vasodilation to the penis and maintains erection. Will not cause an erection unless man is actually aroused
No evidence that it improves sexual function, although could increase duration
May lead to priapism (abnormally long erection) if abused |
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Term
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Definition
Prostaglandin E1
An injection (Caverject®) into penis
A suppository inserted into the urethra (MUSE®)
WILL cause an erection whether intended or not, no further thought required |
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Term
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Definition
Orally active testosterone
Methyl added to C17 for steric hindrance
Chronic use will cause hepatotoxicity |
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Term
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Definition
Orally active testosterone
Methyl added to C17 for steric hindrance
Chronic use will cause hepatotoxicity |
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Term
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Definition
Orally active testosterone
Methyl added to C17 for steric hindrance
Chronic use will cause hepatotoxicity |
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Term
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Definition
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Term
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Definition
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Term
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Definition
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Term
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Definition
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Term
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Definition
| Transdermal testosterone patch |
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Term
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Definition
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Term
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Definition
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Term
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Definition
Fertility Drug
LHRH analog that is given in pulses to mimic the physiologic release and cause release of LH/FSH |
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Term
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Definition
Fertility Drug- An estrogen antagonist
It competes with estrogen for binding sites in the hypothalamus, anterior pituitary and at the ovary. Because it is an antagonist, the hypothalamus senses a low estrogen level and more LHRH is secreted resulting in more FSH and LH.
The increased FSH may result in the development and release of more than one egg—multiple births with fertility drugs |
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Term
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Definition
Emergency Contraception
It is a competitive antagonist at the progesterone receptor.
THIS IS AN ABORTIVE AGENT; used up to 6 weeks after a person’s missed period
If used in later stages (~week 6) must be used with prostaglandin (misoprostol) to cause uterine contractions; late stages must be done under physician supervision |
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Term
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Definition
Emergency Contraceptive
Partial agonist at progesterone receptors (selective progesterone receptor modulator) [SPRM]
Effective for up to 120 hours (5 days)
Inhibits ovulation and prevents implantation (major again) |
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Term
| Plan B® One Step (1.5 mg levonorgestrel) |
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Definition
Emergency Contraception
Inhibits/prevents tubular transport of sperm and ova, makes it very difficult for two to meet and fertilization to occur; changes secretions so movement difficult
Also prevents implantation; considered main mechanism |
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Term
| Next Choice® (0.75 mg levonorgestrel) |
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Definition
Emergency Contraceptive
Inhibits/prevents tubular transport of sperm and ova, makes it very difficult for two to meet and fertilization to occur; changes secretions so movement difficult
Also prevents implantation; considered main mechanism |
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Term
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Definition
Long Acting GNRH Agonist
Given in steady state to desensitize the receptors and therefore decrease LH and FSH release; NOT considered a fertility agent
Specifically for treatment of central precocious puberty;
Also for prostate cancer and endometriosis |
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Term
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Definition
Long Acting GNRH Agonist
Given in steady state to desensitize the receptors and therefore decrease LH and FSH release; NOT considered a fertility agent
Specifically for treatment of endometriosis;
Also for prostate cancer and central precocious puberty |
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Term
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Definition
Long Acting GNRH Agonist
Given in steady state to desensitize the receptors and therefore decrease LH and FSH release; NOT considered a fertility agent
Specifically for treatment of prostate cancer;
Also for endometriosis and central precocious puberty |
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Term
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Definition
Endometriosis Therapy
Decreases the output of FSH and LH and it blocks the synthesis of estrogen and progesterone; It has weak androgenic activity.
Stops the menstrual cycle—essentially puts patient into menopause
Given pre- or post- surgery to limit growth; usually on 3-6 months
Women often experiences androgenic effects—
Facial hair, decreased breast size, weight gain, hot flashes |
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Term
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Definition
(etonogestrel)
Implanted under the skin, inside the upper arm. The implant is effective up to 3 years and fertility is restored promptly after removal |
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Term
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Definition
(medroxyprogesterone acetate)
Patient loses menstrual cycle but will have spotting or irregular cycle at first
Used in males who are sex offenders to inhibit LH and FSH for the subsequent reduction in testosterone and spermatogenesis (called Chemical Castration) |
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Term
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Definition
Selective Estrogen Receptor Modulator
2nd generation
(Estrogen) Antagonist in breast tissue
Antagonist in uterine tissue—removes increased risk of uterine cancer
Agonist in bone—prevents osteoporosis |
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Term
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Definition
Selective Estrogen Receptor Modulator
1st generaion
(Estrogen) Antagonist in breast tissue—used to treat breast cancer
Agonist in bone—helps prevent osteoporosis
Agonist in uterus—increased risk of uterine cancer |
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Term
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Definition
Estrogen used in OC's
Dose is 10-50 micrograms, usual range is 20-35 micrograms |
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Term
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Definition
Estrogen in OC's
Prodrug of Ethinyl Estradiol
Dose is 10-50 micrograms, usual range is 20-35 micrograms |
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Term
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Definition
| Progesterone with anti-androgenic action |
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Term
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Definition
| Progesterone with anti-androgenic action |
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Term
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Definition
| Progesterone with minimal androgenic activity (0/+) |
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Term
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Definition
| Progesterone with minimal androgenic activity (0/+) |
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Term
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Definition
| Progesterone with minimal androgenic activity (0/+) |
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Term
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Definition
| Progesterone with minimal androgenic activity (0/+) |
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Term
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Definition
| Progesterone with (++) androgenic activity |
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Term
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Definition
| Progesterone with (++) androgenic activity |
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Term
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Definition
| Progesterone with most (+++) androgenic activity |
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Term
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Definition
| Progesterone with most (+++) androgenic activity |
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Term
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Definition
Syndrome of inappropriate antidiuretic hormone (SIADH) Therapy
Vasopressin Antagonists
V1/V2 antagonist |
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Term
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Definition
Syndrome of inappropriate antidiuretic hormone (SIADH) Therapy
Vasopressin Antagonists
Selective V2 antagonist |
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Term
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Definition
Syndrome of inappropriate antidiuretic hormone (SIADH) Therapy
MOA: inhibit postsynaptic (2nd messenger/enzyme mechanism) of V2 receptors |
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Term
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Definition
Syndrome of inappropriate antidiuretic hormone (SIADH) Therapy
MOA: inhibit postsynaptic (2nd messenger/enzyme mechanism) of V2 receptors |
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Term
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Definition
(dDAVP)
Vasopressin Agonist
Used for the treatment of central Diabetes Insipidus |
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Term
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Definition
Induce or augment labor in the last trimester
Promote milk letdown
Dosed intranasally
Reduce or prevent postpartum hemorrhage
Making uterus firm or contracted reduces bleeding; single IM injection |
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Term
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Definition
Hyperprolactinemia Treatment
Selective Dopamine (D2) agonist
Advantage is only need to dose 1-2x per week, very long acting
SE= Decreased nausea and vomiting SE
But can produce heart valve problems with chronic use |
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Term
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Definition
Hyperprolactinemia Treatment
Somewhat selective Dopamine (D2) agonist
Old-fashioned
Must dose 2-3 times per day
SE= Headache, nausea, vomiting - severe/substantial side effects
First dose phenomenon so take at bed |
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Term
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Definition
Recombinant human IGF-1
Necessary for treatment of Laron Dwarfism, only therapy that works |
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Term
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Definition
GH Replacement
Identical to human GH; come from “biotech” engineering
Dosed daily with sc injections and continue until age 18 when epiphyses close
Works to treat primary and hypothalamic dwarfism |
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Term
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Definition
Treatment for Excess GH
GH receptor antagonist
Binds to the GH receptor but does not activate the JAK-STAT signaling pathway.
Concern: decrease GH receptor activation could increase AP tumor size |
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Term
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Definition
Treatment for Excess GH
Somatostatin Analog |
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Term
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Definition
Treatment for Excess GH
Somatostatin Analog |
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Term
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Definition
Treatment for Excess GH
Somatostatin Analog |
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Term
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Definition
Treatment for Excess GH
Somatostatin Analog |
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Term
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Definition
GHRH Replacement therapy
Synthetic GHRH, first 29 AA’s of natural GHRH
Diagnostic to test AP function or to treat hypothalamic dysfunction
Receptors for GHRH are located in the Anterior Pituitary (AP)
Drug does not work if problem is with receptors in AP |
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Term
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Definition
Inactive corticoid that must be metabolized
Short acting
Equal g-coid and m-coid affinity |
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Term
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Definition
| Short acting corticoid with more m-coid activity |
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Term
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Definition
Intermediate acting corticoid with slightly more g-coid activity
Used for anti-inflammatory and immunosuppressive properties |
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Term
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Definition
Inactive
Intermediate acting corticoid with slightly more g-coid activity
Used for anti-inflammatory and immunosuppressive properties |
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Term
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Definition
Intermediate acting corticoid with slightly more g-coid activity
Used for anti-inflammatory and immunosuppressive properties |
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Term
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Definition
Intermediate acting
Only active at g-coid receptors
More toxic |
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Term
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Definition
Long acting corticoid
Only active at g-coid receptors
Used for anti-inflammatory and immunosuppressive properties |
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Term
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Definition
Long acting corticoid
Only active at g-coid receptors
Used for anti-inflammatory and immunosuppressive properties |
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Term
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Definition
Short acting corticoid
Much more active at m-coid
Used for mineralocorticoid effects |
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Term
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Definition
Endogenous mineralocorticoid
No glucocorticoid effects |
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Term
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Definition
| Alpha2 Agonist that can be used as a non-hormonal treatment for vasomotor spasms |
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Term
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Definition
Progestin only contraception
Primary action is inhibition of ovulation via negative feedback to hypothalamus (GnRH) and anterior pituitary (FSH and LH). It also acts by altering the endometrium - it becomes less receptive to implantation - and the cervical secretions become thick (decreases sperm motility) |
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Term
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Definition
primary androgen
goes on to form testosterone |
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Term
| Glucocorticoid mechanism of action to reduce inflammation |
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Definition
Induce synthesis of annexins which inhibit phospholipase A2.
Phospholipase A2 catalyzes production of arachidonic acid, precursor of prostaglandins and leukotrienes—pro-inflammatory
Glucocorticoids can treat all causes of inflammation—invading pathogen, physical trauma, inappropriate immune response—do not need to identify type |
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Term
| Mechanism of Glucocorticoid Immunosuppression |
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Definition
| Inhibits production of cytokines—specifically Interleukins and TNFα |
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