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Endo-Repro Drugs > Diabetes Drugs > Flashcards

Diabetes Drugs Flashcards

1
Q

Normal Insulin Profile

A
  • Low basal rate + higher stimulated Rate
  • Insulin T1/2 = 3-5 hrs, degraded by kidney + liver
  • Endogenous Insulin: 60% liver metab, 40% kidney Metab. (prox. tubules)
  • Exogenous Insulin: 60% kidney metab, 40% liver Metab
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2
Q

Regular Insulin- SubQ

A
  • Short Acting
  • Soluble crystalline Zn2+ form of recombinant human insulin
  • Hexamerizes at injection site
  • Effects in 30 min; Peak @ 2-3 hrs; T1/2 = 5-8 hrs
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3
Q

Regular Insulin- IV

A
  • Short Acting
  • Diluted, phosphate buffered, no Zn2+
  • Forms monomers instantly following IV
    Key in crisis situations i.e. DKA
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4
Q

Neutral Protamine Hagedorn (Isophane) Insulin (NPH)

A
  • Intermediate Acting
  • Combines insulin (-) and protamine (+) s/t neither is uncomplexed (isophane)
  • Protamine degrades to release insulin after SubQ injection
  • Onset 2-5 hrs; Duration 4-12 hrs
  • Highly unpredictable action
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5
Q

Rapid Acting Insulin Analogs (drugs + properties)

A
  • Human insulin analogs

- Onset 5-15 min; Peak @ 1 hr; Duration

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6
Q

Glargine

A
  • long acting human insulin analog
  • Crystallization into slowly dissolving hexamers upon injection
  • Slow onset: 1-1.5 hrs, Max. effect 4-6 hrs.
  • Maintained 11-24 hrs or longer; 1x daily injection
  • Provides background (basal) insulin activity
  • Asn at alpha 21 replaced w/ gly; 2 arg added to c-terminus of beta chain
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7
Q

Detemir

A
  • long acting human insulin analog
  • Most reproducible effects of the int. and long acting insulins
  • Onset: 1-2 hrs; Duration > 12 hrs
  • 2x daily dosing for smooth background insulin activity
  • Thr at B30 omitted; C14 fatty acid attached to B29
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8
Q

Degludec

A
  • Ultra long lasting human insulin analog
  • Onset 1-1.5 hrs; Duration up to 42 hrs; 1x daily dosing
  • 1 AA deleted from human insulin and conjugated to hexadecandeioic acid via. y-L-glutamyl spacer at the AA Lys at B29
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9
Q

Afrezza (inhalable Insulin)

A
  • Rapid acting insulin
  • Peak ~15 min.
  • Adv. Effects: couch, throat pain/irritation, hypoglycemia
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10
Q

Insulin Adverse Effects

A

Weight gain: Type 2
Lipodystrophy: injection site fatty tissue hypertrophy
Hypoglycemia: Type 1
Abs: very rare allergy or resistance
- Insulin efficacy may be changed by glucocorticoids, OCPS, B-agonists/antagonists

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11
Q

Metformin

A
  • Biguanide, 1st line Type 2 DM drugs
  • Targets liver, activates AMPK, Mechanisms not fully understood
  • Decreases hepatic glucose output & lowers fasting glucose
  • Anti-Hyperglycemic BUT NOT Hypoglycemic
  • Doesn’t cause weight gain, may help w/ weight loss in obese pt.
  • T1/2: 1.5-3 hrs; excreted unchanged in urine
  • 1st line monotherapy for DM2 + lifestyle changes or in combo with nearly every other DM2 med.
    Adverse Effects:
  • N/V, diarrhea, abdominal discomfort
  • Decreased B12 absorption (screen annually)
  • Severe lactic acidosis: very rare, dose related w/ heaptic or renal insufficiency
    Contraindications: Renal disease, Alcoholism or liver disease, predisposition to tissue anoxia (cardiopulm) – b/c increase risk of lactic acidosis
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12
Q

Insulin Secretagogues

A
  • Sulfonylureas, Meglitinide, Nateglinide
  • Target ATP sensitive K+ channels
  • Action depends on having functional beta- cells
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13
Q

Sulfonylureas

A

Stimulate insulin release from beta-cells
1st gen: Tolbutamide, Chloropromide, Tolazamide (not used)
2nd gen: Glyburide, Glimepiride, Glipizide

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14
Q

2nd Gen. Sulonylureas

A
  • well absorbed, protein-bound in plasma
  • Increased hypoglycemia risk w/ longer half life
    Glyburide: widely prescribed
    Glipizide: Short T1/2, extended release formula widely uesd
    Glimepiride: Longest T1/2, 1x daily dose
    Adverse Effects:
  • Weight gain + hypoglycemia
  • Glyburide + Glipizide: liver + kidney inactivation, contraindicated w/ hepatic and renal dysfunction
  • Glimepiride: liver inactivation, not indicated w/ hepatic disease
    Drug interactions:
  • Decreased efficacy w/ CYP3A4 activators (barbituates, rifampin)
  • Decreased efficacy w/ OCPs, Glucocorticoids, Phenytoin, thiazides & beta-agonists
  • Tolerance: decreased efficacy w/ years of tx, secondary failure
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15
Q

Repaglinide

A

Meglinitide

  • structurally unrelated to sulfonylureas but same mech- stimulate insulin release form beta-cells
  • Rapid abs, short T1/2, fast/brief insulin stimulation
  • Take before meals to decrease post-prandial hyperglycemia
  • T1/2: 1 hr, peak: 30-60 min
  • Caution w/ heapatic/renal impairment
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16
Q

Nateglinide

A
  • D- Phe derivative
  • Even faster and shorter duration
  • Liver inactivation- caution w/ liver disease, safe w/ very reduced renal function
  • May cause weight gain
17
Q

Thiazolidinediones (glitazones)

A

Pioglitazone & Rostiglitazone
- PPARy agonists: PPARy is a nuclear factor that increases transcription of genes encoding proteins that mediate insulin action
- Increase glucose uptake in adipose (primary target), muscle and liver in response to insulin
- Decrease visceral fat deposits, increase FA uptake at other sites
- Benefits take weeks-months
Adverse Effects:
- modest weight gain w/ some fluid retention
- Changes in HDL, LDL and TGs
- Mild anemia
- Risk of fatal liver damage- contraindicated w/ hepatic disease, do liver function test w/ initial tx
Drug interactions: - metab by CYP3A4, may induce enz. that degrade OCPs
Rostiglitazone: BLACK BOX WARNING
- May induce CHF w/ acute MI
- Limit to pt. already on Rostiglitazone or whose sugar can’t be controlled any other way

18
Q

GLP-1 & DPP-4

A

GLP-1: Glucagon- like peptide, incretin

  • Released after meals to stimulate insulin secretion
  • Stim. glucose dependent insulin secretion and inhibits glucagon release
  • Delays gastric emptying, normalizes fasting/post-prandial insulin

DPP-4: Dipeptidyl Peptidase IV

  • Rapidly inactivates GLP-1; T1/2= 1-2 min
  • Increases insulin and speeds up gastric emptying by inhibiting GLP-1 action
19
Q

GLP-1 Receptor Agonists

A

Exenatide, Liraglutide, Dulaglutide, Albiglutide
- Peptide agonists of GLP-1, DPP-4 resistant
- SubQ, monotherapy or in combo w/ other drugs
- Don’t cause weight gain, may cause weight loss
Exenatide: 2x/daily
Liraglutide: 1x/daily
Dulaglutide: 1x/weekly
Albiglutide: 1x/weekly, T1/2= 5-8 days
Adverse Effects:
- N/V, Diarrhea
- may increase hypglycemic episodes when used w/ sulfonylureas (increase insulin release/activity)
- Cleared by kidney- contraindicaed w/ renal insufficiency

20
Q

DPP-4 Inhibitors

A

Sitagliptin, Saxagliptin, Linaglipitin, Alogliptin
- Small molecule DPP-4 inhibitors: increase GLP-1 and GIP levels which stimulates insulin secretion, suppresses glucagon production and slows gastric emptying
Sitagliptin & Saxagliptin: Renally excreted; dose adjust for renal dysfunction
- Saxagliptin = CYP3A4/5 metab.; Sitagliptin not CYP metab

21
Q

SGLT-2 Inhibitors

A

Canaglifozin, Dapaglifozin, Empagliflozin
- Inhibitors of SGLT-2: kidney Na/Glucose co-transporter
- Decreases glucose reabs and increases glucose excretion
Contraindications: Type 1 DM or DKA
- Severe renal impairment, ESRD, Dialysis
Adv. Effects: - UTIs and vag. yeast infections
- Diuretic effect – orthostatic hypotension, dizziness, fainting (most common in 1st 3 mo.)

22
Q

alpha- glucosidase Inhibitors

A

Acarbose + Miglitol
Acarbose: complex oligosacch. or microbial origin
Miglitol: simple sugar analog
- competitively inhibit alpha-glucosidases in intestines which digest dietary starches into absorbable monosacch
- Decreases upper intestinal digestion of starch and disaccharides, defers to SI
- Decreases post-prandial glucose spike
- No hypoglycemia when used alone, little effect on weight
- Decreases Hb1AC but not as well as metformin or sulfonylureas
Adverse Effects:
- Abdominal pain, diarrhea
- Gass b/c of carb. fermentation
- Contraindicated w/ GI disease

23
Q

Pramlintide

A

Amylin: secreted by beta-cells, slows gastric emptying and decreases glucagon production
Amylin Agonist: slows gastric emptying, increases satiety, suppresses post-prandial plasma glucagon and hepatic glucose output
- Adjucnt tx of DM Type 1 & 2
- SubQ; may cause weight loss
Adverse Effects: Nausea, Hypoglycemia
- Contraindicated in patients w/ gastroparesis or other GI motility disorders; caution w/ drugs affecting GI motility

24
Q

Colsevelelam

A

Bile Acid Resin: Cholesterol drug repurposed for DM Type 2
- Modest efficacy, unclear mech.
- Oral admin, no systemic abs, distributed in GI tract
Adverse Effects:
- Contipation, dyspepsia, Abdominal pain, nausea
- Can increase TGs and interfere w/ absorption of commonly used drugs

25
Q

Bromocriptine

A

DA Rec. Agonist

  • Tx for PD and Hyper-PRL repurposed for DM Type 2
  • Modest efficacy

Endo-Repro Drugs (5 decks)

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