Colesevelam

Colesevelam Brand Name– WelChol

What is Colesevelam

Colesevelam hydrochloride is a bile acid sequestrant used for the treatment of hypercholesterolemia and diabetes mellitus.

It is an oral, non-absorbed hydrogel polymer that has a high capacity to bind bile acids.

When used as a single agent in adults with hypercholesterolemia, colesevelam reduces LDL-cholesterol by roughly 15 to 20%, compared with 30% reductions typically seen with HMG-CoA reductase inhibitors as monotherapy.

In children with heterozygous familial hypercholesterolemia (n = 128), colesevelam reduced LDL-cholesterol by approximately 13% and increased high-density lipoprotein cholesterol by approximately 6% after 8 weeks of therapy.

The effects of colesevelam on LDL-cholesterol are synergistic with those of HMG-CoA-reductase inhibitors.

Colesevelam effectively lowers both LDL- and total cholesterol in a dose-dependent fashion.

Colesevelam may be administered concurrently with HMG-CoA reductase inhibitors. When colesevelam is used in combination with fenofibrate in adults, serum triglyceride concentrations have been reported to increase by 6%.

In 3 randomized, placebo-controlled, 26-week clinical trials in adult patients with type 2 diabetes, colesevelam, when added to existing diabetes therapies, significantly decreased hemoglobin A1C by 0.5% as compared to placebo; fasting plasma glucose concentrations decreased by approximately 14 mg/dL.

Indications

  1. hypercholesterolemia
  2. hyperlipoproteinemia
  3. type 2 diabetes mellitus

For the treatment of primary hypercholesterolemia

for use as adjunctive therapy to diet and exercise for the reduction of elevated LDL cholesterol in patients with primary hyperlipoproteinemia as monotherapy or in combination with an HMG-CoA reductase inhibitor

Side Effects

  1. asthenia
  2. back pain
  3. bradycardia
  4. constipation
  5. dyspepsia
  6. dysphagia
  7. elevated hepatic enzymes
  8. fatigue
  9. folate deficiency
  10. GI obstruction
  11. headache
  12. hemorrhoids
  13. hypertension
  14. hypertriglyceridemia
  15. hypoglycemia
  16. infection
  17. influenza
  18. myalgia
  19. myocardial infarction
  20. nausea
  21. pancreatitis
  22. pharyngitis
  23. rash
  24. rhinitis
  25. vomiting

Monitoring Parameters

  • serum cholesterol profile
  • serum creatinine/BUN
  • serum triglycerides

Contraindications

  • biliary obstruction
  • breast-feeding
  • children
  • cholelithiasis
  • coagulopathy
  • constipation
  • dysphagia
  • gastroparesis
  • GI obstruction
  • hemorrhoids
  • hypertriglyceridemia
  • ileus
  • infants
  • malabsorption syndrome
  • neonates
  • pancreatitis
  • phenylketonuria
  • pregnancy
  • surgery
  • vitamin A deficiency
  • vitamin D deficiency
  • vitamin K deficiency

Interactions

  • Acebutolol
  • Acetohexamide
  • Alendronate; Cholecalciferol
  • Alogliptin; Metformin
  • Amlodipine; Hydrochlorothiazide, HCTZ; Olmesartan
  • Amlodipine; Olmesartan
  • Ascorbic Acid, Vitamin C
  • Atorvastatin; Ezetimibe
  • Atropine
  • Atropine; Benzoic Acid; Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate
  • Atropine; Difenoxin
  • Atropine; Diphenoxylate
  • Atropine; Edrophonium
  • Atropine; Hyoscyamine; Phenobarbital; Scopolamine
  • Belladonna Alkaloids; Ergotamine; Phenobarbital
  • Bempedoic Acid; Ezetimibe
  • Bendroflumethiazide; Nadolol
  • Brimonidine; Timolol
  • Bupivacaine; Lidocaine
  • Calcium; Vitamin D
  • Canagliflozin; Metformin
  • Carbamazepine
  • Chenodiol
  • Chlorpropamide
  • Cholic Acid
  • Class IA Antiarrhythmics
  • Clobazam
  • Clonazepam
  • Clorazepate
  • Cranberry, Vaccinium macrocarpon Ait.
  • Cyanocobalamin, Vitamin B12
  • Cyclosporine
  • Dapagliflozin; Metformin
  • Deferasirox
  • Diazepam
  • Digoxin
  • Diltiazem
  • Dorzolamide; Timolol
  • Drospirenone; Ethinyl Estradiol
  • Drospirenone; Ethinyl Estradiol; Levomefolate
  • Empagliflozin; Linagliptin; Metformin
  • Empagliflozin; Metformin
  • Encainide
  • Ergocalciferol, Vitamin D2
  • Ertugliflozin; Metformin
  • Ethinyl Estradiol
  • Ethinyl Estradiol; Desogestrel
  • Ethinyl Estradiol; Ethynodiol Diacetate
  • Ethinyl Estradiol; Etonogestrel
  • Ethinyl Estradiol; Levonorgestrel
  • Ethinyl Estradiol; Levonorgestrel; Ferrous bisglycinate
  • Ethinyl Estradiol; Levonorgestrel; Folic Acid; Levomefolate
  • Ethinyl Estradiol; Norelgestromin
  • Ethinyl Estradiol; Norethindrone
  • Ethinyl Estradiol; Norethindrone Acetate
  • Ethinyl Estradiol; Norethindrone Acetate; Ferrous fumarate
  • Ethinyl Estradiol; Norethindrone; Ferrous fumarate
  • Ethinyl Estradiol; Norgestimate
  • Ethinyl Estradiol; Norgestrel
  • Ethotoin
  • Ezetimibe
  • Ezetimibe; Simvastatin
  • Fat soluble vitamins
  • Felbamate
  • Fish Oil, Omega-3 Fatty Acids (Dietary Supplements)
  • Flecainide
  • Folic Acid, Vitamin B9
  • Fosphenytoin
  • Gabapentin
  • Gemfibrozil
  • Glimepiride
  • Glimepiride; Pioglitazone
  • Glimepiride; Rosiglitazone
  • Glipizide
  • Glipizide; Metformin
  • Glyburide
  • Glyburide; Metformin
  • Hydantoins
  • Hydrochlorothiazide, HCTZ; Olmesartan
  • Hydroxocobalamin
  • Insulins
  • Lamotrigine
  • Levetiracetam
  • Levothyroxine
  • Levothyroxine; Liothyronine (Porcine)
  • Levothyroxine; Liothyronine (Synthetic)
  • Lidocaine
  • Lidocaine; Prilocaine
  • Linagliptin; Metformin
  • Liothyronine
  • Lomitapide
  • Lorazepam
  • Lovastatin; Niacin
  • Mephobarbital
  • Mestranol; Norethindrone
  • Metformin
  • Metformin; Pioglitazone
  • Metformin; Repaglinide
  • Metformin; Rosiglitazone
  • Metformin; Saxagliptin
  • Metformin; Sitagliptin
  • Mexiletine
  • Moricizine
  • Mycophenolate
  • Nadolol
  • Niacin, Niacinamide
  • Niacin; Simvastatin
  • Obeticholic Acid
  • Olmesartan
  • Oxcarbazepine
  • Pentobarbital
  • Phenobarbital
  • Phenytoin
  • Phytonadione, Vitamin K1
  • Primidone
  • Propafenone
  • Pyridoxine, Vitamin B6
  • Secobarbital
  • Segesterone Acetate; Ethinyl Estradiol
  • Succinimides
  • Sulfonylureas
  • Tetracyclines
  • Theophylline, Aminophylline
  • Thyroid hormones
  • Tiagabine
  • Timolol
  • Tocainide
  • Tolazamide
  • Tolbutamide
  • Trandolapril; Verapamil
  • Ursodeoxycholic Acid, Ursodiol
  • Valproic Acid, Divalproex Sodium
  • Vancomycin
  • Verapamil
  • Vitamin A
  • Vitamin E
  • Warfarin
  • Zonisamide
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