FINAL 02 - Drugs Affecting Hormonal Systems Flashcards
Sulfonylureas and glinides are ___________
Insulin secretagogues
Have a small lipophilic substituent on the para position of the phenyl ring (R1 on the pharmacophore) and an alkyl or cyclic lipophilic substituent on the non-sulfonyl-attached urea nitrogen (R2 on the pharmacophore) (Generations of sulfonylureas)
1st generation
Tolbutamide, chlorpropamide, and acetohexamide are examples of __________ sulfonylureas
1st generation
Replaces the small lipophilic p-substituents found in the first-generation agents by a larger p-(B-arylcarboxyamidoethyl) group (Generations of sulfonylureas)
2nd generation
Glyburide and glipizide are examples of __________ sulfonylureas
2nd generation
Has increased potency, more rapid onset, shorter plasma half-lives, and longer durations of action (Generations of sulfonylureas)
2nd generation
Benzoic acid derivative of the non-sulfonylurea moiety of glibenclamide group (Drugs for diabetes melitus)
Meglitinide/Glinide
Prototype drug of meglitinide/glinides
Meglitinide
Thiazolidinediones are also known as __________
Glitazones
__________ are insulin-sensitizing agents
Biguanides
Incretin system modulating agents are __________ agonists
GLP-1 (Glucagon-like peptide-1)
Incretin system modulating agents are ___________ inhibitors
DDP-IV (Dipeptidyl peptidase type 4)
Vildagliptin and saxagliptin are DDP-IV inhibitors with __________ group
Nitrile/Cyano
Has a piperazine ring fused to a pyrazole in place of the pyrrole ring but still contains the a-amino acyl moiety and the amide bond (Examples of DDP-IV inhibitors)
Sitagliptin
Is a xanthine derivative (Examples of DDP-IV inhibitors)
Linagliptin
A cyclic benzenesulfonamide that closely resembles hydrochlorothiazide (a thiazide diuretic) (Examples of glucose elevating agents)
Diazoxide
Is an ATP-sensitive potassium channel opener (Examples of glucose elevating agents)
Diazoxide
The thyroid contains two hormones, __________ and ______________ (LL)
L-thyroxine (T4), L-triiodothyronine (T3)
Meaning of MIT (Thyroid hormones)
Monoiodotyrosine
Meaning of DIT (Thyroid hormones)
Diiodotyrosine
DIT + DIT = __________
T4
MIT + DIT = __________
T3
A metabolically inactive form of T3
Reverse T3 (rT3)
__________ and __________ are examples of synthetic thyroid hormones (LL)
Levothyroxine sodium, Liothyronine sodium
Contains a mixture of the sodium salts of T4 and T3 in a 4:1 ratio by weight (Examples of synthetic thyroid hormones)
Liotrix
A synthetic (+)-stereoisomer isomer of T4 (Examples of synthetic thyroid hormones)
Dextrothyroxine (dT4, Choloxin)
Drugs used for the treatment of hyperthyroidism (excessive production of thyroid hormones)
Antithyroid drugs
Methimazole and propylthiouracil are __________ (Antithyroid drugs)
Thioamides
Refers to the drug therapies used to treat osteoporosis
Antiresorptive agents
Analogs used for estrogen replacement therapy (Types of antiresorptive agents)
Estrogen analogs
Raloxifene is an example of ___________ (Types of antiresorptive agents)
Selective estrogen receptor modulators (SERMs)
The first SERM approved for the prevention of osteoporosis in postmenopausal women (Examples of SERMs)
Raloxifene
A benzothiophene derivative that is a semi-rigid analog of tamoxigen (Examples of SERMs)
Raloxifene
Lasofoxifene, ospemifene, bazedoxifene, and toremifene are examples of __________ SERMs
2nd generation
___________ have covalent carbon-phosphorus bonds (Types of antiresorptive agents)
Bisphosphonates
Have carbon-oxygen-phosphorus bonds (Types of antiresorptive agents)
Bisphosphates
2 groups of bisphosphonates (NN)
Non-N-containing bisphosphonates, N-containing bisphosphonates
Etidronate and tiludronate are examples of ___________ (Types of bisphosphonates)
Non-N-containing bisphosphonates
Alendronate, pamidronate, risedronate, ibandronate, and zoledronic acid are examples of __________ (Types of bisphosphonates)
N-containing bisphosphonates
Its site of action is the aminoacyl-transverse ribonucleic acid (tRNA) synthase (Types of bisphosphonates)
Non-N-containing bisphosphonates
Its site of action is the farnesyl pyrophosphate synthase (FPPS) (Types of bisphosphonates)
N-containing bisphosphonates
Also known as sCT, miacalcin, and calcimar (Types of antiresorptive agents)
Calcitonin-salmon
A recombinant human parathyroid hormone (PTH) (Types of bone-forming agents)
Teriparatide (hPTH(1-3), Forteo)
Includes sodium fluoride and calcium salts (Types of bone-forming agents)
Inorganic salts
____________ are therapies that include RANKL inhibitors and Cathepsin K inhibitors (Types of bone forming-agents)
Monoclonal antibody-based therapies
Denosumab is a ___________ (Types of monoclonal antibody-based therapies)
RANKL inhibitor
Odanacatib is a __________ (Types of monoclonal antibody-based therapies)
Cathepsin K inhibitor
Is classified as both an antiresoprtive agent and a bone-forming agent (Drug therapies used to treat osteoporosis)
Strontium ranelate
Paricalcitol and doxercalciferol are drugs based on __________ (Drug therapies used to treat hyperparathyroidism)
Vitamin D2 (Ergocalciferol)
A calcimimetic; is used to activate the calcium sensing receptor (CaSR) (Drug therapies used to treat hyperparathyroidism)
Cinacalcet
A parathyroid hormone also known as rDNA 1-84 (Drug therapy used in the treatment of hypoparathyroidism)
Preos
2 drug therapies used to treat hypercalcemia of malignancy (BG)
Bisphosphonates, Gallium nitrate
Zoledronic acid and pamidronate are examples of ___________ (Drug therapies used to treat hypercalcemia of malignancy)
Bisphosphonates