MCPC IRAT/GRAT Non-insulin T2DM Drugs

Metformin brand name

Glucophage, Glumetza, Riomet

Metformin drug class

Antidiabetic Agent, Biguanide

Metformin MOA

Decreases hepatic glucose production, decreases intestinal absorption of glucose and improves insulin sensitivity (increases peripheral glucose uptake and utilization)

Tolbutamide brand name

Orinase

Tolbutamide drug class

1st generation sulfonylureas

Tolbutamide MOA

-block efflux of K+ from beta-islet cells > increase calcium influx > insulin granule exocytosis = increased insulin levels.

-reduces serum glucagon indirectly via insulin and somatosin release which inhibits alpha islet cell activity

Tolazamide brand name

Tolinase

Tolazamide drug class

sulfonylureas

Tolazamide MOA

-block efflux of K+ from beta-islet cells > increase calcium influx > insulin granule exocytosis = increased insulin levels.

-reduces serum glucagon indirectly via insulin and somatosin release which inhibits alpha islet cell activity

Chlorpropamide brand name

Diabinese

Chlorpropamide drug class

sulfonylureas

Chlorpropamide MOA

-block efflux of K+ from beta-islet cells > increase calcium influx > insulin granule exocytosis = increased insulin levels.

-reduces serum glucagon indirectly via insulin and somatosin release which inhibits alpha islet cell activity

Glipizide brand name

Glucotrol XL, Glucoctrol

Glipizide drug class

sulfonylurea

Glipizide MOA

Stimulates insulin release from the pancreatic beta cells; reduces glucose output from the liver; insulin sensitivity is increased at peripheral target sites

Glimepiride brand name

Amaryl

Glimepiride drug class

Sulfonylurea

Glimepiride MOA

Stimulates insulin release from the pancreatic beta cells; reduces glucose output from the liver; insulin sensitivity is increased at peripheral target sites

Glyburide brand name

Diabeta, Glynase, Micronase

Glyburide drug class

sulfonylurea

Glyburide MOA

Stimulates insulin release from the pancreatic beta cells; reduces glucose output from the liver; insulin sensitivity is increased at peripheral target sites

Pioglitazone brand name

Actos

Pioglitazone drug class

Thiazolidinediones

Pioglitazone MOA

Thiazolidinedione antidiabetic agent that lowers blood glucose by improving target cell response to insulin, without increasing pancreatic insulin secretion. It has a mechanism of action that is dependent on the presence of insulin for activity. Pioglitazone is a potent and selective agonist for peroxisome proliferator-activated receptor-gamma (PPARgamma). Activation of nuclear PPARgamma receptors influences the production of a number of gene products involved in glucose and lipid metabolism. PPARgamma is abundant in the cells within the renal collecting tubules; fluid retention results from stimulation by thiazolidinediones which increases sodium reabsorption.

Rosiglitazone brand name

Avandia

Rosiglitazone drug class

Thiazolidinedione

Rosiglitazone MOA

Thiazolidinedione antidiabetic agent that lowers blood glucose by improving target cell response to insulin, without increasing pancreatic insulin secretion. It has a mechanism of action that is dependent on the presence of insulin for activity. Rosiglitazone is an agonist for peroxisome proliferator-activated receptor-gamma (PPARgamma). Activation of nuclear PPARgamma receptors influences the production of a number of gene products involved in glucose and lipid metabolism. PPARgamma is abundant in the cells within the renal collecting tubules; fluid retention results from stimulation by thiazolidinediones which increases sodium reabsorption.

Troglitazone brand name

Rezulin

Troglitazone drug class

Thiazolidinediones

Troglitazone MOA

agonize PPAR-gamma (peroxisome proliferator-activated receptor gamma)

Exenatide brand name

Byetta, Bydureon, Bcise

Exenatide drug class

GLP-1 agonist

Exenatide MOA

-agonize the GLP-1 receptor > increase insulin release and decrease glucagon release in a glucose-dependent manner

-also delays gastric emptying and improves satiety

Dulaglutide brand name

Trulicity

Dulaglutide drug class

GLP-1 agonist

Dulaglutide MOA

-agonize the GLP-1 receptor > increase insulin release and decrease glucagon release in a glucose-dependent manner

-also delays gastric emptying and improves satiety

Semaglutide brand name

Ozempic and Rybelsus

Semaglutide drug class

GLP-1 agonists

Semaglutide MOA

-agonize the GLP-1 receptor > increase insulin release and decrease glucagon release in a glucose-dependent manner

-also delays gastric emptying and improves satiety

Liraglutide brand name

Victoza

Liraglutide drug class

GLP-1 agonist

Liraglutide MOA

-agonize the GLP-1 receptor > increase insulin release and decrease glucagon release in a glucose-dependent manner

-also delays gastric emptying and improves satiety

Tirzepatide brand name

Mounjaro

Tirzepatide drug class

GLP-1/GIP agonist

Tizeaptide MOA

-agonize the GLP-1 receptor and GIp receptors > increase insulin release and decrease glucagon release in a glucose-dependent manner

Sitagliptin brand name

Januvia

Sitagliptin drug class

Dipeptidyl Peptidase-4 inhibitor (DPP-4i)

Sitagliptin MOA

DPP-4 degrades incretin hormones in the body. DPP-4i prevent the enzyme DPP-4 from breaking down: incretin hormones, glucagon-like peptide 1 (GLP-1), glucose-dependent insulinotropic polypeptide (GIP)

Saxagliptin brand name

Onglyza

Saxagliptin drug class

DPP-4i

Saxagliptin MOA

DPP-4 degrades incretin hormones in the body. DPP-4i prevent the enzyme DPP-4 from breaking down: incretin hormones, glucagon-like peptide 1 (GLP-1), glucose-dependent insulinotropic polypeptide (GIP)

Linagliptin brand name

Tradjenta

Linagliptin drug class

DPP-4i

Linagliptin MOA

DPP-4 degrades incretin hormones in the body. DPP-4i prevent the enzyme DPP-4 from breaking down: incretin hormones, glucagon-like peptide 1 (GLP-1), glucose-dependent insulinotropic polypeptide (GIP)

Alogliptin brand name

Nesina

Alogliptin drug class

DPP-4i

Alogliptin MOA

DPP-4 degrades incretin hormones in the body. DPP-4i prevent the enzyme DPP-4 from breaking down: incretin hormones, glucagon-like peptide 1 (GLP-1), glucose-dependent insulinotropic polypeptide (GIP)

Canagliflozin brand name

Invokana

Canaglifozin drug class

SGLT2-inhibitors (sodium-glucose co-transporter 2 inhibitor)

Canagliflozin MOA

-In the proximal renal tubule SGLT2-I reabsorbs glucose from the lumen.

-inhibiting SGLT2 reduces the reabsorption of glucose which increases renal glucose excretion and decreases plasma glucose concentration

Dapagliflozin brand name

Farxiga

Dapagliflozin drug class

SGLT2-i

Dapagliflozin MOA

-In the proximal renal tubule SGLT2-I reabsorbs glucose from the lumen.

-inhibiting SGLT2 reduces the reabsorption of glucose which increases renal glucose excretion and decreases plasma glucose concentration

Empagliflozin brand name

Jardiance

Empagliflozin drug class

SGLT2-i

Empagaliflozin MOA

-In the proximal renal tubule SGLT2-I reabsorbs glucose from the lumen.

-inhibiting SGLT2 reduces the reabsorption of glucose which increases renal glucose excretion and decreases plasma glucose concentration

Ertugliflozin brand name

Steglatro

Ertugliflozin drug class

SGLT2-i

Ertugliflozin MOA

-In the proximal renal tubule SGLT2-I reabsorbs glucose from the lumen.

-inhibiting SGLT2 reduces the reabsorption of glucose which increases renal glucose excretion and decreases plasma glucose concentration

Sotagliflozin brand name

Inpefa

Sotagliflozin drug class

SGLT2-inhibitor

Sotagliflozin MOA

Sotagliflozin is an inhibitor of sodium-glucose cotransporter (SGLT) 1 and 2. SGLT2 inhibition reduces renal reabsorption of glucose and sodium, which may decrease cardiac preload/afterload and downregulate sympathetic activity. SGLT1 inhibition reduces intestinal absorption of glucose and sodium. The mechanism for sotagliflozin's cardiovascular benefits has not been established.

Gabapentin brand name

Gabarone; Gralise; Neurontin; Relgaabi

Gabapentin drug class

antiseizure agent, GABA analog

Gabapentin MOA

Gabapentin is structurally related to GABA. However, it does not bind to GABAA or GABAB receptors, and it does not appear to influence degradation or uptake of GABA. High affinity gabapentin binding sites have been located throughout the brain; these sites correspond to the presence of voltage-gated calcium channels specifically possessing the alpha-2-delta-1 subunit. This channel appears to be located presynaptically, and may modulate the release of excitatory neurotransmitters which participate in epileptogenesis and nociception. These effects on restless leg syndrome are unknown.

Amitriptyline brand name

Elavil

Amitriptyline drug class

TCA antidepressant

Amitriptyline MOA

Increases the synaptic concentration of serotonin and/or norepinephrine in the central nervous system by inhibition of their reuptake by the presynaptic neuronal membrane pump.

Nortriptyline brand name

Pamelor

Nortriptyline drug class

TCA

Nortriptyline MOA

Traditionally believed to increase the synaptic concentration of serotonin and/or norepinephrine in the central nervous system by inhibition of their reuptake by the presynaptic neuronal membrane. Inhibits the activity of histamine, 5-hydroxytryptamine, and acetylcholine. It increases the pressor effect of norepinephrine but blocks the pressor response of phenethylamine. However, additional receptor effects have been found including desensitization of adenyl cyclase, down regulation of beta-adrenergic receptors, and down regulation of serotonin receptors.

Duloxetine brand name

Cymbalta

Duloxetine drug class

SNRI

Duloxetine MOA

Duloxetine is a potent inhibitor of neuronal serotonin and norepinephrine reuptake and a weak inhibitor of dopamine reuptake. Duloxetine has no significant activity for muscarinic cholinergic, H1-histaminergic, or alpha2-adrenergic receptors. Duloxetine does not possess MAO-inhibitory activity.

Venlafaxine brand name

Effexor

Venlafaxine drug class

SNRI

Venlafaxine MOA

Venlafaxine and its active metabolite, O-desmethylvenlafaxine (ODV), are potent inhibitors of neuronal serotonin and norepinephrine reuptake and weak inhibitors of dopamine reuptake. Venlafaxine and ODV have no significant activity for muscarinic cholinergic, H1-histaminergic, or alpha2-adrenergic receptors. Venlafaxine and ODV do not possess MAO-inhibitory activity. Venlafaxine functions like an SSRI in low doses (37.5 mg/day) and as a dual mechanism agent affecting serotonin and norepinephrine at doses above 225 mg/day (Harvey 2000; Kelsey 1996).

Desvenlafaxine brand name

Pristiq, Khedezla

Desvenlafaxine drug class

SNRI

Desvenlafaxine MOA

Desvenlafaxine is a potent and selective serotonin and norepinephrine reuptake inhibitor.

fluconazole oral brand name

Diflucan

Fluconazole drug class

Azole antifungal

Fluconazole MOA

Interferes with fungal cytochrome P450 activity (lanosterol 14-α-demethylase), decreasing ergosterol synthesis (principal sterol in fungal cell membrane) and inhibiting cell membrane formation

Nystatin oral brand name

DOM-Nystatin [DSC]; JAMP-Nystatin; PMS-Nystatin; TEVA-Nystatin

Nystatin drug class

antifungal

Nystatin MOA

Binds to sterols in fungal cell membrane, changing the cell wall permeability allowing for leakage of cellular contents

Terconazole cream brand name

TARO-Terconazole

Terconazole drug class

Azole antifungal

Terconazole MOA

Terconazole is a triazole ketal antifungal agent; involves inhibition of fungal cytochrome P450. Specifically, terconazole inhibits cytochrome P450-dependent 14-alpha-demethylase which results in accumulation of membrane disturbing 14-alpha-demethylsterols and ergosterol depletion.