Management and Pharma DM Flashcards by whitney hohman

Insulin
MOA, Indications, Side Effects

Exist as dimer & monomers –> monomers absorbed more rapidly
Admin 20 min prior to meal
Hypoglycemia

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Neutral Protamine Hagedorn (NPH) Insulin

MOA, Indications, Side Effects

Complexed w/ protamine (+charge) –> higher order structure –> slows dissociation & rate of absorption

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Rapid-acting Insulin

MOA, Indications, Side Effects

Insulin lispro, Insulin aspart, Insulin glulisine

Take at meal or w/in 5-10 min of meal

Rapid onset, limited duration

A little better hypoglycemia & HbA1c than insulin

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Long-acting Insulin

Insulin glargine

MOA, Indications, Side Effects, Contraindications

Altered aa sequence –> shift isoelectric point–> less soluble –> formation of crystals

100: same insulin, less volume

300: more stable, absorbed slower

DM1/DM2
A bit better hypoglycemia & HbA1c than NPH
Only admin subcutaneously otherwise severe hypoglycemia

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Insulin lispro

Fast acting insulin

Pro –> lys/pro

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Insulin aspart

Fast acting insulin

Pro –> asp

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Insulin glulisine

Fast acting insulin

Pro –> glu

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Insulin glargine-yfgn

MOA, Indications, SE, contraindications

Long-acting insulin

Interchangeable w/ insulin glargine (lower cost alternative)

DM1/DM2
A bit better hypoglycemia & HbA1c than NPH
Only admin subcutaneously otherwise severe hypoglycemia

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Insulin detemir

MOA, Indications, SE, contraindications

Long acting

Fatty acid (myristic acid) facilitates i/a w/ serum binding proteins (albumin) –> albumin slowly releases insulin

DM1/DM2
A bit better hypoglycemia & HbA1c than NPH
Only admin subcutaneously otherwise severe hypoglycemia

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Insulin degludec

MOA, Indications, SE, contraindications

Long-acting

More complex insulin –> slows down rate creating dimers –> monomers

DM1/DM2
A bit better hypoglycemia & HbA1c than NPH
Only admin subcutaneously otherwise severe hypoglycemia

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Metformin

MOA, Indications, SE, contraindications

Decreases hyperglycemia w/o stimulating insulin secretion & reduced potential for hypoglycemia

Decrease hepatic glucose production

Increase sk mm glucose uptake & incorporation into glycogen

Inhibits mitochondrial respiration –> decreases energy available –> metabolic flux –> metabolic response (increase insulin sensitivity, decrease gluconeogenesis)

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Metformin

Indications, SE, contraindications

First line DM2
GI upset (diarrhea), Lactic Acidosis
HF/Decreased kidney fxn/IV contrast

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Secretagogues (sulfonylurea derivatives)

MOA, SE, Contraindications

Bind & block K+ channel –> cell depolarizes –> Ca2+ influx –>insulin release

Increase insulin secretion

SE: WT gain, hypoglycemia

C: Sulfa allergy

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First generation secretagogues

Tolbutamide, Chlorpropamide, Toazamide

Longer t1/2, greater incidence of hypoglycemia, more frequent drug i/a

decrease fasting/postprandial glucose

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Second generation secretagogues

Glyburide, Glipizide, Glimepiride

Rapid onset of action, better coverage of postprandial glucose rise –> preferred b/c can be taken once daily

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(Me)glitinides, Repaglinide, Nateglinide

MOA, SE, Contraindication

M: Similar MOA as sulfonylyurea –> weakly binds SUR1 of ATP-activated K+ channel

SE: Hypoglycemia (less likely) 2/2 delayed meals, increased physical activity, renal insufficiency

Con: Renal Insufficiency

Thiazolidinediones (TZDs),
Rosiglitazone,
Pioglitazone

MOA

Ligand for peroxisome proliferator – activated receptor gamma (PPARy) in adipocytes –> TFs that regulate card/lipid metabolism

Increase insulin sensitivity (adiponectin)

Decrease glucose by increase fat storage

Thiazolidinediones (TZDs),
Rosiglitazone,
Pioglitazone

SE, Contraindication

SE: WT gain, edema, bone frx

C: Heat failure

SGLT2 Inhibitors: Gliflozin

MOA

Inhibit SGLT2 –> increased excretion of glucose

Efficacy linked to kidney fxn

SGLT2 Inhibitors: Gliflozin

Indications, SE, Contraindications

I: Cardioprotective –> first line for CVD/HF

SE: WT loss, UTI, Hypotension, Thrist, DKA, Limb amputation

C: Low renal fxn

Incretins: GIP

MOA

Produced in K cells of small intestine

“Obese hormone” fats increased secretion

GIP levels high in DM2

Incretins: GLP-1 agonist (semaglutide w/ SNAC)

MOA

Produced from proglucagon in L cells of small intestine –> stimulates glucose-dependent insulin release from pancreatic islets

Portective/proliferative effect on B-cells

Increased satiety signal

Decreased gastric emptying

Incretins (GIP, GLP-1)

Indications, AE

I: Heart –> cardioprotective
BV–> vasodilation
Atherosclerosis

WT loss (GLP-1/GIP dual)

AE: Long-term effects signaling by decreasing GIP receptors

Incretin effect –> greater release of insulin when oral> IV

Dipeptidyl Peptidase-4 (DPP-4) Inhibitors

MOA

-glipton

Inactivates GLP-1 & GIP

Decreases glucagon secretion

Increase insulin secretion (weaK)

Dipeptidyl Peptidase-4 (DPP-4) Inhibitors AE, Contraindication

AE: Overall, well-tolerated, GI upset (common), Joint pain (rare), Increased risk HF hospitalization (saxa & alo), increased angioendema w/ ACE/ARB C: family Hx of Thyroid CA --> increases risk for it No MENS2 pt

Amylin -- Pramlintide MOA

Modifications make pramlintide soluble & non-self aggregating Decrease glucagon secretion during a meal Decrease food emptying from stomach --> curbs appetite

Amylin

-- Pramlintide

Amylin -- Pramlintide Indications AE

1. Adjunct in pts who take insulin w/ meals 2. Moderate WT loss in obese pts w/o diabetes

a-glucosidase inhibitors

Acarobose Miglitol

a-glucosidase inhibitors MOA

Decrease intestinal absorption of starch, dextrin, disaccharidases Increase Incretin release

a-glucosidase inhibitors Indications AE

1. Adjunct to diet & exercise as monotherapy when other oral antidiabetic agents CI Combo w/ oral antidiabetic drugs & insulin in DM2 2. Flatulence, diarrhea, Abd bloating

Phentermine MOA

Sympathomimetic structurally similar to amphetamine --> reduces appetite & increases metabolism via stimulation of norepinephrine release

Phentermine Indications AE Contraindications

1. SHORT-TERM ONLY (<12 wks) 2. HTN/Tachy/increased CV events/arrhythmias Serotonin Syndrome (w/ MOAI) 3. DO NOT USE w/ MOA-I

Topiramate MOA

Reduce appetite & increases satiety w/ blocking voltage gated Na+ channels & enhancing GABA(A)

Topiramate Indications AE Contraindications

1. +Phentermine Can be used in pt w/ szr hx Long-term therapy >12 wks 2. Cog impairment, birth defects, acute angle glaucoma 3. Pregnancy

Orlistat MOA

Gastric & pancreatic lipase inhibitor --> decreased fat absorption (~30% reduction)

Orlistat Indications AE Contraindications

1. Long-term therapy (>12 wks) 2. Steatorrhea, fat soluble viatmin deficiency, GI upset, Hepatotoxic, Cholelithiasis 3. Pregnancy

Naltrexone/ Bupropion MOA

Unknown Naltrexone: pure opioid antagonist Bupropion: weak dopamine/NE reuptake inhibitor

Naltrexone/ Bupropion Indications AE Contraindications

1. Long-term therapy (>12 wks) 2. Elevated BP, decrease szr threshold, BBW: suicidal ideation, acute angle glaucoma 3. Opiod use, hx of szr, uncontrolled HTN