Pramlintide — pharmacology
Molecular targets, mechanism of action, pharmacokinetics and interactions as characterised in humans.
§2Pharmacology
§2.1Molecular targets
Table 2. Molecular targets recorded for Pramlintide, with the character of the interaction and the potency where the Institute holds it.
| Target | Interaction | Note |
|---|---|---|
| Amylin receptors (AMY1–AMY3) | Agonist | Retains native amylin receptor activity |
| Calcitonin receptor (CTR) | Agonist | Component of the amylin receptor complex |
§2.2Mechanism of action
Pramlintide reproduces the postprandial actions of endogenous amylin, which is deficient in insulin-deficient diabetes: it slows gastric emptying, suppresses inappropriate postprandial glucagon secretion, and promotes satiation. It has no effect on insulin secretion and is therefore used as an adjunct to insulin rather than as a secretagogue.[1,2]
§2.3Pharmacokinetics
- Terminal half-life
- ≈48 min
- Time to maximum concentration
- ≈20 min
- Volume of distribution
- not extensively distributed
- Plasma protein binding
- ≈40 %
- Clearance
- ≈1 L/min
- Bioavailability
- 30–40 % absolute
Renal metabolism with the principal metabolite des-lys pramlintide retaining activity. Not recommended in severe renal impairment.
§2.4Interactions
- Insulin — mandatory prospective dose reduction
- Any oral medicine dependent on rapid absorption should be taken at least one hour before or two hours after
- Anticholinergics compound the gastric-emptying delay
References cited on this page
References are numbered in order of first citation in this document. Each superscript in the text links to its entry below.
- Hollander PA, Levy P, Fineman MS, Maggs DG, Shen LZ, Strobel SA, Weyer C, Kolterman OG. Pramlintide as an adjunct to insulin therapy improves long-term glycemic and weight control in patients with type 2 diabetes: a 1-year randomized controlled trial. Diabetes Care 2003;26(3):784–790. doi:10.2337/diacare.26.3.784 · PMID 12610038
- Lau DCW, Erichsen L, Francisco AM, Satylganova A, le Roux CW, McGowan B, Pedersen SD, Pietiläinen KH, Rubino DM, Batterham RL. Once-weekly cagrilintide for weight management in people with overweight and obesity: a multicentre, randomised, double-blind, placebo-controlled and active-controlled, dose-finding phase 2 trial. The Lancet 2021;398(10317):2160–2172. doi:10.1016/S0140-6736(21)01751-7 · PMID 34798060
Identifiers are reproduced only where the Institute holds them. Where a digital object identifier or PubMed identifier is not shown, the Institute has recorded the journal and year and has not constructed an identifier.