Term
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Definition
Selective Estrogen Receptor Modulator (SERM):
agonist in some tissues antagonist in others
Partial agonist: stimulates estrogen receptors in bone, but inhibits in other tissues
Effects on bone similar to estrogen: Decrease resorption of bone, Decrease bone turnover, Increase bone mineral density
Contraindications: Pre-menopausal, Pregnancy , Concurrent estrogen therapy, History of breast cancer
Adverse Effect: Increase risk of deep vein thrombosis (DVT |
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Term
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Definition
"nates" and reclast
used in Osteoporosis, Decrease the incidence of fractures
. They inhibit enzyme systems that are involved in bone resorption
Mechanism of Action: Inhibition of farnesyl diphosphate synthase
Reduction of geranylgeranyl diphosphate
Decrease of GTPase prenylation, Osteoclast inactivation, Osteoclast apoptosis, Inhibition of osteoclast formation
Paget’s Disease: Reduce bone turnover rate, Slow disease progression |
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Term
| Finasteride*, Dutasteride (Avodart) |
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Definition
5 α-reductase: converts testosterone to dihydroxytestosterone:
-Mediator of the actions of the hormone
-Testosterone can be aromatized to estrogen, DHT cannot
Competitive inhibitor of 5-α reductase:
Benign prostatic hypertrophy (*Proscar, Avodart),
Alopecia (*Propecia)
Adverse Effects: Diminished libido,erectile dysfuntion
Teratogenicity (woman who are or may become pregnant |
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Term
| Methyltestosterone (Android), Axiron, Androgel |
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Definition
Androgen Replacement
Indications: delayed puberty in males, breast cancer, therapy after testicular cancer, Low testosterone
Controversial indications:
enhancement of athletic performance, female hypo-gonadism, male contraception, catabolic and wasting states (cancer, AIDS), blood dyscrasias |
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Term
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Definition
testosterone to dihydrotestosterone (active form)
Dihydrotestosterone bonds to its receptor and is transported to the nucleus
Initiates transcription of androgen dependent genes |
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Term
| Oral contraceptive Types: |
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Definition
Monophasic: Fixed dose of hormones throughout month
Biphasic: Fixed dose of estrogen, progesterone dose increases during month
Triphasic: Varying amounts of hormones during the month
Progesterone is present to protect the endometrium from estrogen effects: endometrial cancer |
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Term
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Definition
human parathyroid hormone derivative
regulation of bone metabolism, renal tubular reabsorption of calcium and phosphate, and intestinal calcium absorption
Rare risk of osteosarcoma |
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Term
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Definition
| Facilitates absorption of calcium and phosphate from the small intestine |
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Term
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Definition
Anti-RANKL monoclonal antibody
RANKL stimulates osteoclast precursors to form mature osteoclasts.
Used in osteoporosis |
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Term
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Definition
Pre-menopausal women: Birth control, Adolescents when puberty is absent
Post-menopausal women: Prevention of osteoporosis related fractures, Vasomotor symptoms
Controversial in women over 60: May promote CVD, breast cancer, stroke, DVT |
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Term
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Definition
Insulin
-Hexamers and dimers bind 300 times weaker
-Injected 15 minutes before eating
-Peak action in minutes rather than 2 hours
-Duration of action is less than one hour instead of several hours as with regular
-Reduces after meal hyperglycemic episodes and hypoglycemia later |
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Term
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Definition
Lispro (Humalog)
Glulisine (Apidra)
Aspart (NovoLog)
Big advantage: shorter onset than regular insulin
This means better hyperglycemic control after meals |
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Term
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Definition
Synthetic long lasting insulin that binds to albumin via a fatty acid linkage
Slow absorption and longer duration of action (up to 24 hours)
Indicated for basal therapy in type 1 with a once or twice daily dosing and as add on therapy in type 2
No drug interactions with other protein bound drugs
Binds to serum proteins and is slowly released
No drug interactions because is tightly bound |
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Term
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Definition
pH=4
Causes more pain at injection site
Acidic solution is neutralized in body
Insulin precipitates into crystals
Slowly absorbed over 24 hours
Given once daily at bedtime
Insulin precipitates slowly into crystals
Painful injections due to low pH |
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Term
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Definition
-Neuroendocrine hormone
-Synthesized by pancreatic beta cells
-Glucose control after meals
-Slows gastric emptying
-Suppresses glucagon secretion
-Suppression of endogenous glucose output from liver
-Centrally mediated modulation of appetite
-Highly amyloidogenic
-Insulin and Amylin secretion in non-diabetic Adults |
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Term
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Definition
Used only in combination with insulin in type I and type II diabetes
Synthetic analog of amylin
Type 1 or Type 2 (with insulin)
Glucose control after meals
Decreases glucose levels in the 3 hours after meals
Provides a more “tight” control of glucose levels
Given by injection before meals
Markedly less amyloidogenic
Patients have to be motivated
Test glucose before and after every meal and at bedtime
Participate in diabetes education
Understand how to adjust dose of both insulin and Symlin |
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Term
Exenatide (Byetta)
Victoza (liraglutide) |
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Definition
Incretin Mimetic
-Insulin responses to oral glucose are higher than that of iv glucose
Incretin hormones: Intestinal peptides, Glucagon-like peptide 1 (GLP-1)
Mechanism: Stimulation of insulin secretion and sensitivity, Glucose dependent synthesis of insulin, Increase beta cell mass, Increase satiety (reduce food intake), Promote weight loss
Slows gastric emptying- drug interactions
Used only in Type 2 Diabetes
Extended t1/2 compared to GLP-1
Synthetic analog of GLP-1
Type 2 only
1st phase insulin response |
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Term
| Oral Hyperglycemic Agents |
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Definition
Sulfonylureas
Biguanides
Thiazolidinediones
α glycosidase inhibitors
Dipeptide peptidase 4 (DPP-4) inhibitors |
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Term
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Definition
Glyburide (DiaBeta), Glipizide (Glucotrol)
Mechanism: Stimulate insulin release by blocking ATP dependent K+ current in pancreatic β cells
Adverse Effects: Hypoglycemia, Nausea and vomiting, weight gain
For type II
Drug interactions: Increase Effect (hypoglycemia)
Azole antifungals, Salicylates, ASA, Sulfonamides, NSAIDS, Tricyclic Antidepressants
Corticosteroids decrease effects |
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Term
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Definition
Biguanides: First line therapy for Type II Diabetes
Mechanism of action: Inhibition of hepatic glucose production (hepatic gluconeogenesis).
Pharmacological Effects: Decrease hepatic gluconeogenesis, Improve tissue sensitivity to insulin, Decrease peripheral glucose uptake, Decrease intestinal absorption of glucose |
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Term
| Pioglitazone (Actos), Rosiglitazone (Avandia) |
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Definition
Thiazolidinediones, PPARg agonists
Mechanism: Post-receptor insulin mimetic activity affecting insulin receptor kinase activity and insulin receptor phosphorylation
Pharmacological Effects: Increase insulin sensitivity of tissues
Metabolized by p450s, interact with ketoconazole
Increase a person's risk of CHF
83,000 major heart problems since 1999
Might be taken off market
Increase the body's tendency to accumulate fluids due to inadequate pumping from the heart |
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Term
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Definition
α glucosidase inhibitors
Competitive and reversible inhibitor of α glucosidase, hydrolase, pancreatic α amylase
Delay in the breakdown of carbohydrates to glucose
Carbohydrates accumulate in large intestine and local flora cause flatulence and diarrhea |
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Term
| Sitagliptin (Januvia); Linagliptin (Tradjenta) |
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Definition
Slows the inactivation of incretin hormones by inhibiting DPP-4
Incretin hormones (GLP-1): Stimulation of insulin secretion, Glucose dependent synthesis of insulin, Short t1/2, Inactivated by DPP-4 |
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Term
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Definition
MOA:Closes ATP dependent K+ channels in β cells
PCOL effect: Stimulates release of insulin
Gemfibrozil, Clarithromycin, azole antifungals increase effects (block metabolism) |
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Term
| Levothyroxine T4 (Synthroid) |
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Definition
hypothyroid
Hypothyroidism can lead to exaggerated response to CNS depressants, like narcotics and benzos |
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Term
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Definition
Radioactive Iodine
Drug is concentrated in thyroid, where the β particles destroy the gland
Propylthiouracil:
Inhibits thyroid peroxidase, an enzyme responsible for the synthesis of thyroid hormones |
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Term
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Definition
Lethargy
Fatigue
Loss of energy/ambition
Decreased appetite
Increase weight
Intolerance to cold temps |
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Term
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Definition
Insulin binds to tyrosine kinase growth factor receptor
Kinase cascade causes translocation of glucose transporter
Glucose transporter fuses with the membrane
Increased glucose uptake |
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Term
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Definition
| sweating, weakness, tremor, confusion, blurred vision, altered behavior |
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Term
| levothyroxine (T4, Synthroid) MOA: |
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Definition
| activates t4 receptors on end-target cells |
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Term
MOA of finasteride (Propecia, Proscar)
dutasteride (Avodart) |
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Definition
| 5 a-reductase inhibitors. 5 a-reductase converts testosterone to DHT which is active form. |
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Term
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Definition
| inhibition of farnesyl diphosphate synthase, reduction of geranylgeranyl diphosphate, decrease of GTPase prenylation. Osteoclast inactivation. |
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Term
| insulin binds to_____________ receptor which casuses _________ |
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Definition
- tyronsine kinase growth factor
-kinase cascade causes translocation of glucose transporter increased glucose uptake from bloodstream |
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Term
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Definition
| inhibition of gluconeogenesis in the liver, type II only. |
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Term
| ThiaZOlidinedioNES and MOA |
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Definition
"zone" pioglitazone (Actos), rosiglitazone (Avandia)
PPAR-gamma agonists; post-receptor insulin mimetic which affects insulin receptor kinase activity and insulin receptor phosphorylation |
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Term
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Definition
| competitive and reversible inhibitor of alpha-glucosidase hydrolase & pancreatic alpha-amylase |
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Term
| dipeptidyl pePTidase (DPP-4) INhibitor |
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Definition
"ptin"
sitagliptin (Januvia)
linagliptin (Tradjenta) |
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Term
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Definition
| Slows the inactivation of incretin hormones by inhibiting DPP-4 |
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Term
| diabetes can present orally as: |
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Definition
infection
poor wound healing
increased caries risk
candidiasis
gingivitis
periodontitis |
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Term
| clinical guidelines for pts with diabetes: |
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Definition
appointments after a meal
appointments in the morning
gentle handling of tissue
no aspirin with sulfonamides
hypoglycemic episodes are more dangerous than hyperglycemic episodes; keep glucose tablets handy |
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Term
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Definition
prostaglandin analog
Agonists at PGE2 and PGI2 receptors
used in peptic ulcer disease, indicated for administration with NSAIDs |
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Term
| Proton pump inhibitors work by |
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Definition
binding covalently to H+K+aTPase pump
long half life, new pump must be synthesized. |
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Term
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Definition
| Proton pump inhibitor, OTC |
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Term
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Definition
competitively inhibiting histamine 2 receptor.
block gastric acid secretion. |
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Term
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Definition
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Term
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Definition
aluminum hydroxide and sulfated sucrose
- in acid forms suspension that binds ulcer site
- gastro-protective, very safe, not absorbed. |
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Term
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Definition
buffer or neutralize acid. decrease pepsin activity.
Four primary compounds:
sodium bicarb (contraindicated in low salt diet)
magnesium salts
aluminum salt
calcium carbonate (TUMS)
Calcium or magnesium antacids decrease action of tetracycline |
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Term
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Definition
Mechanism: Central dopamine receptor antagonist, promotes motility
Contraction of gastric muscle relaxation of pyloric and duodenal segments increase peristalsis
Adverse Effects: dry mouth, nausea |
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Term
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Definition
Alkylating Agents
Mechanism: Form alkyl radicals that covalently bind with nucleophiles
Phosphate, sulfhydryl, hydroxyl, carboxyl, amino or imidazole groups
React with RNA, DNA, proteins Also, cross link DNA strands
Cyclic nitrogen mustard
Uses: Induction, maintenance, and remission in non-Hodgkins lymphoma, leukemia, prostate, lung, breast, ovarian carcinomas
Severe rheumatoid arthritis, allograft rejection, immune disorders |
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Term
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Definition
Platinum Complex
MOA: produces inter-strand and intra-strand cross-links in DNA
INDICATION: carcinoma of the testis and ovary, bladder neoplasia, head & neck cancer, lung cancer
ADVERSE EFECTS:severe emesis, nephrotoxicity w/ renal tubular necrosis, hearing loss, perhipheral neuropathy |
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