ENDOCRINE PHARMACOLOGY Flashcards
(168 cards)
1
Q
All mediate their ultimate effects by regulating the production
by peripheral tissues of other hormones EXCEPT
A
PROLACTIN
2
Q
Hormones secreted by the Posterior Pituitary are: (2) Take note that both are potent ??
A
Vasopressin
& Oxytocin
VASOCONSTRICTORS
3
Q
Growth Hormone
(GH,
Somatotropin)
Target organ hormone/mediator?
A
Insulin-like
growth factor-1
(IGF-1)
4
Q
Thyroidstimulating
hormone
(TSH)
Target organ hormone/mediator?
A
Thyroxine,
Triiodothyronine
5
Q
Target organ mediator or hormone of Adrenocorticotropi
n
(ACTH)
A
Glucocorticoids,
Mineralocorticoids
, Androgens
6
Q
MOA: DOPAMINE AGONIST, hence inhibiting prolactin
release from the pituitary gland.
Also slightly inhibits GH release.
Dopaminergic effects on CNS motor control and
behavior
A
BROMOCRIPTINE, PERGOLIDE, CABERGOLINE, QUINAGOLIDE
*All are Preg Cat B
7
Q
MOA: Activates oxytocin receptors. Stimulates uterine
contraction and labor. Stimulates mammary glands,
lactation and milk let-down.
A
Oxytocin [X], Demoxytocin
8
Q
Contraindications to oxytocin include
A
fetal distress,
prematurity, abnormal presentation, CPD and
predispositions for uterine rupture
9
Q
is an oxytocin receptor blocker (not yet FDA
approved since there is concern about increased rates
of infant death)
A
ATOSIBAN
10
Q
is an agonist of peripheral Oxytocin
receptors
A
CARBETOCIN
11
Q
MOA: Desmopressin relatively
selective for V2
receptors. Vasopressin V2
receptor agonist which
causes insertion of water
channels in the collecting
duct leading to more water
reabsorption → decrease
the excretion of water; Act
on extra-renal V2 receptors
to increase Factor VIII and
VWF factor
A
DESMOPRESSIN, VASOPRESSIN/ ADH
12
Q
MOA: Antagonist at V1a, V2
receptors. Increases renal
excretion of water in
conditions associated with
increased vasopressin
(like in SIADH)
A
CONIVAPTAN,
TOLVAPTAN, LIXIVAPTAN
13
Q
Used for: Central diabetes
insipidus, Hemophilia A,
von Willebrand’s
disease, Esophageal
variceal bleeding, Primary
nocturnal enuresis
(pediatric Px), colon
diverticula
A
DESMOPRESSIN
Vasopressin/ADH
14
Q
Used in: SIADH, Hyponatremia in
hospitalized patients,
offset fluid retention in
acute heart failure and
SIADH which causes
hyponatremia (dilutional)
A
CONIVAPTAN,
TOLVAPTAN, LIXIVAPTAN
15
Q
ADH ANTAGONIST THAT IS MORE SELECTIVE FOR V2 RECEPTORS?
A
TOLVAPTAN
16
Q
MOA: Increases release of IGF-1 in the liver and cartilage.
Stimulates skeletal muscle growth, amino acid transport,
protein synthesis and cell proliferation.
A
SOMATROPIN
17
Q
Most notable SE of somatropin?
A
Hyperglycemia
18
Q
Same as somatropin. But no release of IGF-1 because it’s
IGF that you gave already.
RECOMBINANT IGF-1
A
MECASERMIN
19
Q
Most notable side effect of MECASERMIN?
A
Hypoglycemia,
20
Q
PEGVISOMANT MOA?
A
Blocks GH receptor
21
Q
Drug for acromegaly?
A
PEGVISOMANT
22
Q
MOA? Suppresses the release of growth hormones, glucagon,
insulin, gastrin, IGF-1, serotonin and gastrointestinal
peptides
A
OCTREOTIDE, LANTREOTIDE
23
Q
Most notable SE of OCTREOTIDE, LANTREOTIDE?
A
biliary sludge and
gallstones
24
Q
Octreotide is the most widely used somatostatin analog,
(how many times??) more potent than somatostain in GH inhibition
A
45x
25
All gonadotropin related drugs are Pregnancy Category (?)
X
26
in women, (?)directs follicle development, whereas (? and?) collaborate in regulating ovarian steroidogenesis
FSH
FSH AND LH
27
in men, (?)regulates spermatogenesis, whereas (?) stimulates
androgen production
FSH, LH
28
Ovulation Induction Protocol??? (3)
* endogenous gonadotropin production is inhibited by
administration of a GnRH agonist or antagonist
* follicle development is driven by daily injections of a
preparation with FSH activity (menotropins, FSH, FSH analog)
* final stage of oocyte maturation is induced with an injection of
LH or hCG to mimic the LH surge
29
Complications of Ovulation Induction?
* multiple pregnancies
* ovarian hyperstimulation syndrome
o syndrome of ovarian enlargement, ascites, hypovolemia and
possibly shock
30
MOA? FOLLITROPIN ALFA, MENOTROPINS (hMG),
UROFOLLITROPIN, FOLLITROPIN BETA
Activates FSH receptors. Mimics effects of endogenous FSH.
31
CHORIOGONADOTROPIN ALFA,
HUMAN CHORIONIC GONADOTROPIN (hCG),
MENOTROPINS (hMG), LUTROPIN ALFA
Activates LH receptors. Mimics endogenous LH.
32
are mixtures of FSH and LH from
postmenopausal women
MENOTROPINS
33
is a recombinant hCG (recall
my previous note that the B-subunits of LH and hCG are
nearly identical)
Choriogonadotropin alfa
34
Synthesis and Transport of Thyroid Hormones? (4 steps)
TRANSPORT
IODINE ORGANIFICATION
COUPLING
PROTEOLYSIS
35
What happens in IODINE ORGANIFICATION phase of Thyroid Synthesis?
o tyrosine residues in thyroglobulin are iodinated to form
monoiodotyrosine (MIT) or diiodotyrosine (DIT)
35
What happens in TRANSPORT phase of Thyroid Synthesis?
o iodide ion is converted to iodine by thyroid peroxidase (TPO)
36
What happens in IODINE COUPLING phase of Thyroid Synthesis?
o 2 molecules of DIT combine to form T4, while 1 molecule each of
MIT and DIT combine to form T3
37
What happens in PROTEOLYSIS phase of Thyroid Synthesis?
o T4 and T3 are released from the thyroid and transported in the
blood by thyroxine-binding globulin (TBG)
38
o sudden acute exacerbation of all of the symptoms of
thyrotoxicosis, presenting as a life-threatening syndrome
THYROID STORM
39
WOLF-CHAIKOFF VS JOD-BASEDOW
* Wolf-Chaikoff effect: ingestion of iodine causes hypothyroidism
* Jod-Basedow phenomenon: ingestion of iodine causes
hyperthyroidism
40
Which drugs inhibit peripheral
conversion of T4 to T3?
Propylthiouracil, Propranolol
Hydrocortison
41
What drugs can cause druginduced
hyperthyroidism?
(CAM)
Clofibrate, Amiodarone, Methadone
42
TREATMENT of:
hyperthyroidism either through an iodine-induced mechanism in
persons with an underlying thyroid disease or through an
inflammatory mechanism that causes leakage of thyroid hormone
TREATMENT: thioamides or corticosteroids
43
MOA: * block uptake of iodide by the gland through competitive inhibition of
the iodide transport mechanism. Useful in amiodarone-induced hyperT
* potassium perchlorate is rarely used clinically because it is
associated with aplastic anemia
ANION INHIBITORS: PERCHLORATE (CLO4–), PERTECHNETATE
(TCO4–), THIOCYANATE (SCN–)
44
is preferred in the first trimester and should be replaced
by Methimazole (MMI) after this trimester.
PTU
45
is the mainstay of the treatment of postpartum
hyperthyroidism, in particular during lactation
METHIMAZOLE
46
NOTABLE SIDE EFFECT OF PTU?
AGRAnuLOCYTOSIS
47
are teratogens (causes
Aplasia Cutis Congenita) in the 1st trimester
Methimazole and Carbimazole
48
is the other name of Methimazole
THIAMAZOLE
49
Drug of choice for nonpregnant hyperthyroid Px
because of longer DOA (24h) and increased potency
METHIMAZOLE
50
Notable side effect of MEHITAMZOLE, CARBIMAZOLE?
AGRANULOCYTOSIS, ALTERERD SENSE OF SMELL AND TASTE
51
Administered orally sodium 131I, it is concentrated by the
thyroid and incorporated into storage follicles
Radioactive Iodine (I131) [X]
52
Notable SE of RADIOACTIVE IODINE
Permanent Hypothyroidism
53
Permanent cure of thyrotoxicosis without surgery
RADIOACTIVE IODINE
54
Preparation for thyroidectomy to reduce the size and
vascularity of the thyroid gland, Radiation prophylaxis.
POTASSIUM IODIDE [D], LUGOL’S SOLUTION /
Potassium Iodide Saturated Solution (KISS)
55
NOTABLE SE OF POTASSIUM IODIDE [D], LUGOL’S SOLUTION /
Potassium Iodide Saturated Solution (KISS)
ANGIOEDEMA
56
* Blocks beta-receptors (control HR and other cardiac
abnormalities of severe thyrotoxicosis).
* Inhibits peripheral conversion of T4 into T 3 (Only
Propranolol)
PROPRANOLOL, ESMOLOL, METOPROLOL, ATENOLOL
57
o medical emergency representing the end state of untreated
hypothyroidism
MYXEDEMA COMA
58
Treatment of MYXEDEMA COMA?
o intravenous loading dose of levothyroxine (300–400 mcg),
followed by 50–100 mcg daily
59
MOA: Thyroid receptor agonist
LEVOTHYROXINE (T4) [A],
LIOTHYRONINE (T3) [A], LIOTRIX [A]
60
4 B’s of thyroid hormone
Brain maturation, Bone
growth, Beta-adrenergic effects, and increase in Basal metabolic rate
61
regulate sodium and potassium reabsorption in the collecting
tubules of the kidney
MINERALOCORTICOIDS
62
CONVERTS CHOLESTEROL TO PREGNENOLONE
DESMOLASE
63
GLUCORTICOIDS:
Low Potency (1)
Medium Potency (2)
High Potency (2)
Low potency: Hydrocortisone (cortisol)
Medium potency:
Fluticasone, Mometasone
High-potency:
Desoximetasone, Clobetasol
64
is the prototype glucocorticoid
Hydrocortisone (cortisol)
65
is the glucocorticoid with the highest
anti-inflammatory potency.
BETAMETHOSONE
66
is the mineralocorticoid with the
highest salt-retaining potency
Fludrocortisone
67
Behavioral changes secondary to steroid use is termed
Roid Rage
68
MOA: Inhibits Desmolase, blocking conversion of cholesterol
to pregnenolone. Reduces synthesis of all hormonally
active steroids.
Uses Breast cancer, Cushing
AMINO-glutethimide
69
* Abused by body builders to lower circulating levels of
cortisol in the body and prevent muscle loss
Amino-glutethimide [D]
70
MOA: Inhibits cholesterol side-chain cleavage, cytochrome
P450 enzymes and other enzymes necessary for
synthesis of all steroids
KETOCONAZOLE
71
MOA: Blocks conversion of 11-deoxycortisol to cortisol via
inhibition of 11B-hydroxylase
METYRAPONE
72
MOA: Competitive inhibitor at the GC receptor as well as
progesterone receptor
Also used as an approved abortifacient for medical
abortion (usually together with misoprostol)
MIFEPRISTONE
73
MOA: Strong agonist of
mineralocorticoid receptors and
moderate activation of
glucocorticoid receptors.
Increases Na reabsorption,
K and H excretion
FLUDROCORTISONE [C],
DEOXYCORTICOSTERONE
74
Blocks Aldosterone
receptors
(mineralocorticoid
receptor antagonist)
SPIRONOLACTONE
75
When given continuously:
antifertility (suppresses
gonadal function)
When given pulsatile:
promotes gonadal function
GNRH AGONISTS
END WITH -RELINS (EXCEPT
LEUPROLIDE)
76
Suppresses the LH surge
to prevent premature
ovulation in assisted fertility
GNRH ANTAGONISTS
END WITH -RELIX
(RELIX KA LANG –
77
Used inPalliative therapy of hormone-responsive tumors
(breast or prostate CA), central precocious puberty,
controlled ovarian stimulation, male infertility,
endometriosis, apoplexy and blindness (if given to a
patient with a GnRH-secreting pituitary tumor)
LEUPROLIDE, GONADORELIN, GOSERELIN,
HISTRELIN, NAFARELIN, TRIPTORELIN
78
is a synthetic human GnRH
Gonadorelin
79
MOA: Blocks GnRH receptors.
Reduces endogenous production of LH and FSH
GANIRELIX, CETRORELIX, ABARELIX, DEGARELIX
80
Endogenous hormone that is involved in pubertal changes,
controlling ovulation, preparing the female reproductive tract
for fertilization, acts on lipid and bone metabolism
ESTROGEN
81
Most potent naturally-occurring estrogen is
17B-estradiol >
estrone > estriol
82
Principal source of estrogen in pre menoupausal? in post menopausal?
Principal source in pre-menopausal: ovaries
o Principal source in post-menopausal: adipose tissue
83
is a mixture of conjugated estrogen used in
HRT
PREMARIN
“PREMARIN is from PREgnant MARe’s urine”
84
what carcinoma is seen in daughters of
mothers who took DES
Clear cell vaginal adenocarcinoma
85
is a synthetic steroid with weak estrogenic,
progestogenic and androgenic activity, and hence is an
agonist of the estrogen, progesterone and androgen
receptor. It is primarily used in menopausal hormone
therapy, postmenopausal osteoporosis and endometriosis.
TIBOLONE
86
Give 3 absolute contraindications of oral contraceptives
● Women age >35 years who smoke > 15 cigarettes per day
● Known ischemic heart disease or multiple risk factors for
cardiovascular disease (older age, smoking, diabetes, and
hypertension)
● Past thromboembolic event, stroke or known thrombogenic
mutations
● Complicated valvular heart disease
● Complicated solid organ transplantation
● Hypertension (systolic >160 mmHg or diastolic >100 mmHg)
● Systemic lupus erythematous (positive or unknown
antiphospholipid antibodies
● Cirrhosis, hepatic adenoma or hepatoma
● Pregnancy and early postpartum (<21 days)
● undiagnosed abnormal uterine bleeding
87
Give 3 relative contraindications of oral contraceptives
● Hypertension (adequately controlled or systolic 140-159 or
diastolic 90-99)
● Women receiving anticonvulsant drug therapy
● Women following bariatric surgery (malabsorptive procedure)
88
MOA of Combination Hormonal Contraceptives
MOA of Combination Hormonal Contraceptives
* inhibition of ovulation (the primary action)
* effects on the cervical mucus glands, uterine tubes, and endometrium
that decrease the likelihood of fertilization and implantation
89
Differences between monophasic vs biphasic/triphasic oral contraceptives
● MONOPHASIC
o combination estrogen-progestin tablets that are taken in
constant dosage throughout the menstrual cycle
● BIPHASIC or TRIPHASIC
o combination preparations in which the progestin or estrogen
dosage, or both, changes during the month
o more closely mimics hormonal changes in menstrual cycle
90
what oral contraceptives are recommended for breastfeeding moms since they do not
affect lactation
Progestin only prepartions
91
What oral contraception is used for postcoital contraceptive?
LEVONORGESTREL,
ETHINYL ESTRADIOL + LEVONORGESTREL
92
emergency contraception should be taken until when?
Must be taken within 72 hours of unprotected sexual
intercourse (not effective once implantation has occurred)
93
MOA: Estrogen antagonist actions in breast tissue and CNS.
Estrogen agonist effects in uterus, liver and bone.
TAMOXIFEN
94
Given for breast cancer patients who are ER+ PR+
TAMOXIFEN [D], TOREMIFENE [D]
95
MOA: Estrogen antagonist actions in breast tissue, uterus and
CNS. Estrogen agonist effects in liver and bone.
Increases bone mineral density.
RALOXIFENE
96
RALOXIFENE
97
Acts as antagonist to estrogen receptors in the pituitary →
inhibit negative feedback mechanism by estrogen → leads
to pituitary stimulation causing ↑ LH and FSH
CLOMIPHENE
98
is the enzyme which converts Testosterone to
Estrogen(Estradiol)
AROMATASE
99
Effective against breast cancers that have become
resistant to tamoxifen
ANASTROZOLE [X], LETROZOLE, EXEMESTANE
100
is an IRREVERSIBLE Aromatase inhibitor
Exemestane
101
MOA: Weak cytochrome P450 inhibitor and partial agonist of
progestin and androgen receptors
DANAZOL
102
Pharmacologic antagonist of glucocorticoid and
progesterone receptors
Uses: Medical abortion, Cushing's syndrome
MIFEPRISTONE
103
Complication: failure to induce complete abortion
sepsis d/t unusual organisms (Clostridium sordelli)
what abortifacient has this complication?
MIFEPRISTONE
104
Active form of testosterone?
DIHYDROTESTOSTERONE
105
Give 2 clinical uses of testosterone?
* Replacement therapy in hypogonadism
* Stimulate RBC production in certain anemias
* Promote weight gain in patients with wasting syndromes (e.g.
AIDS patients)
* performance enhancement in athletes
o exploited illicitly to increase muscle bulk and strength
* Effects of androgen: secondary sexual characteristics, fertility
and libido, male pattern baldness, increases muscle mass,
increased RBC production, decreased urea nitrogen excretion,
maintains normal bone density
106
MOA: Competitive antagonist at androgen receptor
Flutamide [D], Bicalutamide, Nilutamide
107
MOA: Antagonist at androgen receptor. Marked progestational
effect that suppresses the feedback enhancement of LH
and FSH.
CYPROTERONE [X], CYPROTERONE ACETATE
108
Inhibits 5á-reductase enzyme that converts testosterone
to dihydrotestosterone
FINASTERIDE [X], DUTASTERIDE
109
is the most potent form of
testosterone, essential in the development of male
secondary sexual characteristics.
Dihydrotestosterone
110
Can be given to counteract flare effect in GnRH agonist
treatment
FINASTERIDE [X], DUTASTERIDE
111
Giving this drug aids in the management of
smooth muscle hypertrophy in the prostate
5-alpha reductase
112
In treating advanced prostate cancer with leuprolide, what can be
given to prevent the initial increase in testosterone?
Finasteride
113
chronic disorder of carbohydrate, fat, and protein metabolism
due to a relative or absolute deficiency in insulin secretory
response
DIABETES MELLITUS
114
o progressive disorder characterized by increasing insulin
resistance and diminishing insulin secretory capacity
o frequently associated with obesity and is much more
common than type 1 diabetes
o usually has its onset in adulthood
TYPE 2 DIABETES
115
Difference in Type 1 and Type 2 in terms of C-peptide
Type 1 DM: no C-peptide. Type 2: have C-peptide
116
* cleavage of proinsulin and cross-linking result in formation of ??? and ???
of insulin and a residual C-peptide
117
C-Peptide is used to? (2)
o differentiate type 1 and type 2 DM
o rule out factitious hypoglycemia
118
MOA: binds to a tyrosine kinase receptor, which phosphorylates itself
and a variety of intracellular proteins when activated by the
hormone
* activation of phoshphatidylinositol-3 kinase pathway and MAP
kinase pathway
INSULIN
119
is also capable of inducing entry of K+ (potassium) into cells
Insulin
Rapid acting insulin has “amino acids” in their name. Lis (lysine) Pro
(Proline). Etc. Because to make them rapid acting, binaliktad yung
positions ng mga amino acid na ito para maging rapid acting.
Glargine sounds like LARGE! Tunog Long yung effect
DeteMIR ends with MIR for Myristic Acid. A fatty acid added to the
structure to make it long acting
120
WHAT STRATEGY:
most physiologic strategy because it copies the body’s
normal production of insulin as closely as possible
o long-acting insulin (BASAL) + short-acting insulin with every
meal (BOLUS)
BASAL BOLUS
121
WHAT STRATEGY:
o fixed amounts of long-acting insulin to be given routinely
o amount of short-acting insulin varied depending on preprandial
CBG
SLIDING INSULIN SCALE
122
period in type 1 DM when exogenous insulin requirements
decrease due to an increase in the endogenous production of
insulin
* initiation of insulin therapy causes activation of residual
pancreatic beta cells
ON INSULIN: HONEYMOON PERIOD
123
Rapid Acting Insulin? (3)
Lispro, Aspart, Glulisine
124
Short Acting Insulin (1)
Regular Insulin
125
Intermediate Acting Insulin
NPH, Lente
126
Long acting insulin (1)
Ultralente
127
Ultra-Long Acting Insulin (3)
Glargine, Detemir, Lantus
128
Who are at Risk for Insulin-related Hypoglycemia (4)
Advanced renal
disease, elderly, children <7 y/o
129
1st generation Sulfonylureas (3)
Chlorpropamide, Tolbutamide, Tolazamide
130
What generation of sulfonylureas: High propensity to cause hypoglycemia especially
among elderly patients that’s why it is seldom used
First Generation
Chlorpropamide, Tolbutamide, Tolazamide
131
Has the lowest risk of developing hypoglycemia since they
have short duration of action
Meglitinide
132
Used in diabetics with sulfa allergies
taken for post-prandial
hyperglycemi
Meglitinide
133
MOA: * reduces postprandial and fasting glucose levels
* activates AMP-stimulated protein kinase leading to inhibition
hepatic and renal gluconeogenesis
BIGUANIDES
134
FIRST LINE: T2DM, also DM Prevention
PCOS, DOC for OBESE Diabetic
METFORMIN
135
Worse SE of Metformin
Worse SE: lactic acidosis
(especially in renally and hepatically impaired patients,
hence contraindicated), Vit B12 malabsorption, weight loss
136
(2) antidiabetic drug that bypass the insulin receptor.
Both of these medications act via gene expression to sensitize tissue
receptor to insulin
Metformin and its cousin Thiazolidinediones bypass the insulin receptor.
Both of these medications act via gene expression to sensitize tissue
receptor to insulin
137
MOA: increase target tissue sensitivity to insulin by activating the
peroxisome proliferator-activated receptor-gamma nuclear
receptor (PPAR-Ɣ receptor)
THIAZOLIDINEDIONES
138
THIAZOLIDINEDIONE that reduces mortality and macrovascular
events (myocardial infarction and stroke)
Pioglitazone
139
MOA: Inhibits intestinal α-glucosidases → reduce conversion
of starch and disaccharides to monosaccharides →
reduce post prandial hyperglycemia
Acarbose, Miglitol, Voglibose
ALPHA-GLUCOSIDASE INHIBITOR
140
MOA: Activates amylin receptors. Reduce post-meal glucose
excursions Suppresses glucagon release. Delays gastric
emptying. Stimulates CNS to reduce appetite (anorectic
effect).
AMYLIN ANALOG: PRAMLINTIDE
141
Most notable SE of exenatide, liraglutide? (GLP-1 AGONIST)
Acute pancreatitis
142
What GLP 1 Agonist has possible thyroid ca risk?
Liraglutide
143
Sitagliptin, Saxagliptin, Linagliptin,
Vildagliptin, Teneligliptin DRUG CLASS?
DPP-4 INHIBITORS
Inhibits dipeptidyl peptidase-4 (DPP-4) that degrades GLP-1
and other incretins → raises circulating GLP-1 levels.
144
Exenatide, Liraglutide,
Lixisenatide, Semaglutide, Dulaglutide DRUG CLASS?
GLP-1 AGONIST
Activates GLP-1 receptors → reduction of post-meal glucose
excursions.
145
Empagliflozin, Dapagliflozin, Canagliflozin DRUG CLASS?
SGLT-2 INHIBITOR
146
MOA of SGLT-2 INHIBITOR?
NA-GLUCOSE CO-TRANSPORTER 2 (SGLT 2)
INHIBITOR → inhibits reabsorption of glucose in the
kidneys back to the blood → excretion of glucose out in
the urine.
147
Most notable SE of SGLT-2 INHIBITOR
strong smell of urine
148
An appetite suppressant which is an
amphetamine derivative. Side effects will be
similar with amphetamine
PHENTERMINE
[X]
149
MOA: Inhibits gastrointestinal and pancreatic lipases. Reduces
absorption of fats
ORLISTAT (XENICAL)
150
Net effect
on serum calcium/phosphate
levels of PTH?
Serum calcium
increased,
serum phosphate
decreased
151
Net effect
on serum calcium/phosphate
levels of Active Vitamin D Metabolites (Calcitriol)
Serum calcium and
phosphate both increased
152
MOA: Interacts selectively with estrogen receptors leading to
inhibition of bone resorption w/o stimulating breast or
endometrial hyperplasia
SERM: RALOXIFENE [X]
153
WHAT HORMONE?
Inhibits calcium excretion, promotes phosphate excretion and
stimulates the production of active vitamin D metabolites
* Promotes bone turnover by increasing the activity of both
osteoblasts and osteoclasts
PARATHYROID HORMONE
154
At high doses, net effect of elevated PTH
is increased bone
resorption via osteoclast activation, hypercalcemia, and
hyperphosphatemia
155
Stimulus for the release of PTH
decreased free ionized calcium
156
MOA: Acts through PTH receptors to produce a net increase
in bone formation, stimulates bone turnover
TERIPARITIDE (RECOMBINANT PTH )
Acts through PTH receptors to produce a net increase
in bone formation, stimulates bone turnover
This is a key difference between endogenous PTH and
Teriparatide: PTH has net bone resorption, Teriparatide
has net bone formation (‘wag malito!)
157
Commonly added to dairy products and other food
products
* Given topically for psoriasis; given with calcium
supplements for osteoporosis
ERGOCALCIFEROL, CHOLECALCIFEROL
158
is a prodrug that is converted in the
liver to 1,25-dihydroxyvitaminD
DOXERCALCIFEROL
159
are analogs of calcitriol
and are used topically for psoriasis and are being
investigated
Paricalcitol, Calcipotriene
160
* Peptide hormone secreted by parafollicular C cells in the thyroid gland
* decreases serum calcium and phosphate by inhibiting bone
resorption and inhibiting renal excretion of these minerals
* bone formation is not impaired initially, but ultimately it is reduced
CALCITONIN
161
MOA: Acts through calcitonin receptors to inhibit bone
resorption
USES: Paget's disease of bone, Hypercalcemia, Osteoporosis,
Tumor marker for thyroid cancer
Calcitonin, Salcatonin
MNEMONIC: Calcitonin means CALCium INside the bone
162
MOA: Suppresses the activity of osteoclasts in part via
inhibition of Farnesyl Pyrophosphate synthesis.
Inhibits bone resorption and secondarily, bone formation
by acting on the basic hydroxyapatite crystal structure
BISPHOSPHONATES: Alendronate, Etidronate, Ibandronate, Pamidronate, Risedronate,
Tiludronate, Zoledronic Acid (Prototype)
163
notable SE of Bisphosphonates?
Esophagitis, Osteonecrosis of the
jaw,
164
MOA: Binds to dietary phosphate and prevents its absorption
Sevelamer
165
MOA: Binds to RANKL and prevents it from stimulating
osteoclast differentiation and function → inhibits bone
resorption
DENOSUMAB
ANTI RANKL MONOCLONAL ANTIBODY
166
MOA: Activated calcium-sensing receptor → Inhibits PTH
secretion
CINACALCET
“Sinakal siya! Patay!, Cinacal siya, PTHay
167
