ENDO Flashcards
Lipase inhibitor
Orlistat
Drugs for obesity are considered effective if theydemonstrate at least a ___ greater reduction in body weight as compared to placebo (no treatment).
5%
Anorexiants (Appetite Supressant) drugs
- Phentermine
- Diethylpropion
- Increases the release of norepinephrine and dopamine from the nerve terminals and inhibits reuptake of these neurotransmitters, thereby increasing levels of neurotransmitters in the brain.
- The increase in norepinephrine signals a “fight-or-flight” response by the body, which, in turn, decreases appetite.
Phentermine
All of the anorexiants are classified as CONTROLLED SUBSTANCES due to_____
potential for dependence or abuse.
Adverse effect of Diethylpropion
- COMMON: dry mouth, headache, insomnia, and constipation
* Increased heart rate and blood pressure
Avoidance of Diethylpropion/Phentermine in patients with
- history of uncontrolled hypertension,
- cardiovascular disease,
- arrhythmias,
- heart failure, or
- stroke.
Concomitant use of anorexiants with _________ should be avoided.
- monoamine oxidase inhibitors (MAOIs) or other
- sympathomimetics should be avoided.
It is indicated for weight loss orweight maintenance and its clinical utility is limited by gastrointestinal adverse effects.
Orlistat
Inhibits gastric and pancreatic lipases, thus decreasing the breakdown of dietary fat into smaller molecules that can be absorbed.
Orlistat
- Most common: gastrointestinal symptoms, such as oily spotting, flatulence with discharge, fecal urgency, and increased defecation
- These effects may be minimized through a low-fat diet and the use of concomitant cholestyramine.
- Contraindicated in pregnancy and in patients with chronic malabsorption syndrome or cholestasis
Orlistat
- Interferes with the absorption of fat-soluble vitamins and β-carotene
- Advise to take a multivitamin supplement that contains vitamins A, D, E, and K and also β-carotene
Orlistat
- A newer serotonin agonist, with selectivity for the 2C serotonin receptor (5-HT2C)
- Used for chronic weight management
- Not used as it causes valvular heart disease
Lorcaserin
Mode of Action: Lorcaserin
- Selectively activates _____
- Stimulates _______ which activate melanocortin receptors
- Decrease in ____
- Discontinue if the px does not lose at least 5% of body weight after____of use
- 5-HT2C receptors
- pro-opiomelanocortin neurons
- appetite
- 12 weeks
The development of life-threatening ______ has been reported with the use of serotonin agonists.
serotonin syndrome or neuroleptic malignant syndrome
Avoid concomitant use with
- selective serotonin reuptake inhibitors,
- serotonin–norepinephrine reuptake inhibitors,
- MAOIs,
- or other serotonergic drugs
Lorcaserin
The combination of phentermine and ___ has been approved for long-term use in the treatment of obesity.
topiramate
Should not be stopped abruptly as SEIZURES may be precipitated
phentermine/topiramate
Adverse Effects of Topiramate
- Cleft palate
- Paresthesias
- Suicidal ideation
- Cognitive dysfunction
A treatment option for patients with a BMI of 40 kg/m2 or greater who instituted but failed an adequate exercise and diet program (with/without adjunctive drug therapy) and who present with obesity-related comorbid conditions, such as hypertension, impaired glucose tolerance, diabetes mellitus, hyperlipidemia, & obstructive sleep apnea
Bariatric Surgery
The 2 major elements of bone, are crucial not only for the mechanical strength of the skeleton but also for the normal function of many other cells in the body.
Calcium and phosphorus
Are primary regulators of calcium and phosphorus
Parathyroid hormone (PTH) and vitamin D
Play secondary roles of regulators of calcium and phosphorus
calcitonin, glucocorticoids, and estrogens
Nonhormonal regulators of bone mineral homestasis
- Biphosphonates
- Fluride
- Calcimimetics
A condition of PTH excess characterized by hypercalcemia, bone pain, cognitive abnormalities, and renal stones.
Hyperparathyroidism
Primary Hyperparathyroidism results from
parathyroid gland dysfunction
Secondary Hyperparathyroidism results from
Chronic kidney disease
A condition of abnormal mineralization of adult bone secondary to nutritional deficiency of vitamin D or inherited defects in the formation or action of active vitamin D metabolites.
Osteomalacia
Abnormal loss of bone with increased risk of fractures, spinal deformities, and loss of stature; remaining bone is histologically normal.
Osteoporosis
A bone disorder, of unknown origin, characterized by excessive bone destruction and disorganized repair.
Complications include skeletal deformity, musculoskeletal pain, kidney stones, and organ dysfunction secondary to pressure from bony overgrowth
Paget’s disease
The same as osteomalacia, but it occurs in the growing skeleton
Rickets
An osteoblast-derived growth factor that stimulates osteoclast activity and osteoclast precursor differentiation
RANK ligand
At the continuous high concentrations seen in hyperparathyroidism, the net effect of elevated PTH is
- increased bone resorption,
- hypercalcemia, and
- hyperphosphatemia.
Recombinant truncated form of PTH, for parenteral treatment of osteoporosis.
teriparatide
In the treatment of secondary hyperparathyroidism associated with chronic kidney disease, ____ reduces PTH levels, corrects hypocalcemia, and improves bone disease
It can also result in hypercalcemia and hypercalciuria through direct effects on intestinal, bone, and renal handling of calcium and phosphate.
calcitriol
Are approved for treatment of secondary hyperparathyroidism in patients with chronic kidney disease.
- doxercalciferol
- paricalcitol
Is approved for topical treatment of psoriasis.
Calcipotriene (calcipotriol)
The primary toxicity caused by chronic overdose with vitamin D or its active metabolites is
- hypercalcemia,
- hyperphosphatemia, and
- hypercalciuria.
The hormone has been used in conditions in which an acute reduction of serum calcium is needed like in Paget’s disease and hypercalcemia.
Calcitonin
Is approved for treatment of osteoporosis and has been shown to increase bone mass and to reduce spine fractures.
Calcitonin
Can prevent or delay bone loss in postmenopausal women. Their action involves the inhibition of PTH-stimulated bone resorption
Estrogens and selective estrogen receptor modulators (SERMs; eg, raloxifene)
Inhibit bone mineral maintenance.
As a result, chronic systemic use of these drugs is a common cause of osteoporosis in adults. However, these hormones are useful in the intermediate-term treatment of hypercalcemia.
glucocorticoids
Short-chain organic polyphosphate compounds that reduce both the resorption and the formation of bone by an action on the basic hydroxyapatite crystal structure.
Biphosphonates
Are used to manage the hypercalcemia associated with some malignancies and to treat Paget’s disease.
It is used commonly to prevent and treat all forms of osteoporosis.
Biphosphonates
Treatment of hypercalcemia associated with Paget’s disease and malignancies.
Pamidronate, zoledronic acid, or etidronate
The primary toxicity of the low oral bisphosphonate doses used for osteoporosis is
gastric and esophageal irritation
A human monoclonal antibody that binds to and prevents the action of RANKL. It inhibits osteoclast formation and activity and can be used for treatment of postmenopausal osteoporosis.
Denosumab
- lowers PTH by activating the calcium-sensing receptor in the parathyroid gland.
- It is used for oral treatment of secondary hyperparathyroidism in chronic kidney disease & for the treatment of hypercalcemia in patients with parathyroid carcinoma.
- Its toxicities include hypocalcemia and adynamic bone disease, a condition of profoundly decreased bone cell activity.
Cinacalcet
An organic ion bound to 2 atoms of strontium, promotes osteoclast apoptosis and increases concentrations of bone formation markers; it is used in Europe for treatment of osteoporosis.
Strontium ranelate
- Is effective in managing the hypercalcemia associated with some malignancies and possibly Paget’s disease.
- It acts by inhibiting bone resorption.
- To prevent nephrotoxicity, patients need to be well hydrated and to have good renal output.
Gallium nitrate
Used to reduce serum calcium and bone resorption in Paget’s disease and hypercalcemia.
plicamycin (mithramycin)
