Relaxin

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Relaxin

Method of action: Miorelaxant

Treatment option:

Medically reviewed

Marina Burgos

Last updated on 10/01/2026

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Relaxin

What is Relaxin? An Overview

Property Description
Active ingredient Relaxin (or Recombinant Human Relaxin-2)
Form Injectable solution
Pharmacological class Peptide Hormone; Anti-fibrotic Agent
General purpose Softens tissue and increases blood flow
Origin Naturally produced human hormone; medicinal form is recombinant (synthetic copy)

What Type of Medicine is Relaxin? (The Core Identity)

Relaxin is a naturally occurring human peptide hormone, scientifically classified as belonging to the insulin-like growth factor (IGF) superfamily of proteins. The active ingredient used in medicine is typically Recombinant Human Relaxin-2 (H2), a form engineered to be structurally identical to the natural hormone. This substance is clinically recognized for its potent effects on connective tissue and the vascular system. Its primary pharmacological roles are as a powerful vasodilator (widening blood vessels) and an anti-fibrotic agent (preventing tissue stiffening), distinguishing it from typical small-molecule drugs.


Form and Composition (The Substance Itself)

Relaxin is typically prepared as a sterile injectable solution because, as a protein, it must be administered directly into the bloodstream to avoid degradation in the digestive system. The dosage form is an injectable solution for administration via either intravenous (IV) infusion or subcutaneous injection. The composition consists of the Relaxin protein suspended in a safe, aqueous base/vehicle. This non-oral delivery method is necessary to ensure the active ingredient remains intact and therapeutically available.


General Therapeutic Purpose (The Connection to Health)

The general purpose of Relaxin is centered on its unique ability to modulate the stiffness of connective tissues and enhance circulation. Its action involves influencing the turnover of collagen, the main structural protein in rigid tissues. Relaxin's anti-fibrotic properties are utilized for their potential to prevent or reverse scarring in various organs. Furthermore, its action as a vasodilator supports improved blood flow. The hormone plays a role in relaxing and expanding arteries, which indicates the substance is effective at opening blood vessels to enhance the delivery of oxygen and nutrients to tissues.

Regulatory References

  1. NIH Classification

What side effects are possible with Relaxin?

Possible Side Effects and Safety Information


The safety profile of Recombinant Human Relaxin-2 (Serelaxin) is fundamentally defined by its documented action as a potent vasodilator (a substance that widens blood vessels). This effect underpins the most frequently observed and most serious documented adverse reactions. The information below reflects safety data reported in official governmental resources and clinical trial summaries.

Classification of Adverse Reactions

The primary system affected by the drug's action is the Vascular System. Adverse reactions are officially categorized by frequency:

  • Common Adverse Reactions: The events most frequently observed in clinical studies include headache and hypotension (low blood pressure). These are the most common official adverse reactions.
  • Other Documented Reactions: Less frequent reactions have been reported across other System-Organ Classes, including Nervous System effects (e.g., dizziness, fatigue) and Gastrointestinal effects (e.g., nausea, vomiting). Infusion site reactions may also occur.

Serious Adverse Reactions and Safety Constraints

The chief high-level safety constraint is the potential for severe hypotension. This risk is specifically documented to be heightened when the medication is administered concurrently with other powerful vasodilators (such as certain PDE5 inhibitors), which can lead to clinically significant drops in blood pressure and the possibility of syncope (fainting).

Contextual Safety Patterns

Given the drug's rapid pharmacological action, adverse reactions like hypotension are typically associated with the start of the intravenous infusion or during periods of dose escalation. Conversely, the drug’s effects decline rapidly upon treatment cessation due to the peptide’s short half-life, which is a key safety characteristic documented in regulatory summaries. Safety reviews have noted that the profile was generally comparable between different adult cohorts, including Older Adults.

Overdose and Emergency Response

Overdose and when to seek help

Official regulatory information regarding Relaxin (Recombinant Human Relaxin-2) overdose is derived from the government regulatory reviews of clinical trials assessing high-dose effects, as a final approved label with a dedicated overdose section is not available.

Overdose manifestations center on an exaggeration of the medicine’s powerful actions on the vascular system. The primary and dose-limiting manifestation is sustained hypotension (low blood pressure). High-dose exposure is also associated with transient, asymptomatic elevations in serum creatinine, indicating potential for dose-related effects on the renal system.

When to Seek Immediate Medical Help

Immediate medical attention is mandatory for signs of severe cardiovascular distress. Regulatory documentation specifies a mandatory threshold for intervention: the infusion must be permanently terminated and urgent care sought if the patient's systolic blood pressure falls below 100 mm Hg in two consecutive measurements.

Overdose Management

  • Antidote: No specific antidote is known or documented in official regulatory sources.
  • Supportive Measures: Management consists of symptomatic and supportive treatment, focused primarily on administering Intravenous (IV) Fluids to address and correct hypotension.
  • Population Note: Patients with pre-existing mild-to-moderate renal impairment may be more susceptible to the dose-limiting renal toxicity observed at supra-therapeutic levels and require close monitoring.

Therapeutic Uses of Relaxin

What Relaxin Treats: Main Uses and Benefits

Relaxin is relevant across domains where additional symptomatic support is needed, focusing on areas of tissue support and circulatory function. It is commonly used across conditions presenting with systemic or localized discomfort.

The primary use is generally in conditions involving episodic or fluctuating manifestations, helping with symptoms related to heightened physiological activity associated with pregnancy and childbirth. It is also relevant in contexts marked by increased discomfort or tension, such as symptoms related to inflammatory or irritative states associated with tissue rigidity and is applied in clinical settings that involve acute or unstable symptom patterns, such as those associated with cardiopulmonary and circulatory issues.

Quick Fact: Support for Symptomatic Periods Relaxin is commonly used when short-term symptomatic assistance is needed in conditions where symptoms create noticeable physiological strain, helping patients cope more steadily with symptom fluctuations.

The medication offers symptomatic relief that helps patients cope more steadily. The support contributes to easing the overall symptom load. It is applied in scenarios where additional management of discomfort is required, and may assist with maintaining functional stability during symptomatic periods.

Eligibility and Restrictions for Use

The official eligibility profile for Relaxin (Serelaxin) is defined by its Non-Approved Regulatory Status in major global jurisdictions. Regulatory authorities, including the European Medicines Agency and the U.S. Food and Drug Administration, have not granted a marketing authorization for the medicine, which means no patient population is eligible for its use under a standard, government-approved label. Consequently, no official contraindications are documented.


Eligibility Scope

Category Official Regulatory Statement / Trial Data Restriction
Populations for whom use is allowed None. Not approved for standard labeled use.
Age-related eligibility rules Restricted to the Adult population (ge 18 years). Pediatric use is not established.
Condition-specific eligibility rules Severe Renal Impairment (eGFR below 25 mL/min/1.73 m^2) and Known Hepatic Impairment were trial exclusions, limiting the available data set.
Pregnancy and lactation eligibility status Use Not Established. No official regulatory statement is available.

Connection to the Overall Eligibility Profile

The entire patient population is ineligible for standard prescription use due to the official refusal of marketing authorization based on regulatory review. The only available eligibility constraints are those derived from the clinical trials, which limit the data set to adults without severe organ dysfunction.

What should I know about interactions with other medicines?

Interactions with other medicines and products

The interaction profile for Relaxin (Recombinant Human Relaxin-2), a peptide hormone, is defined by its strong physiological effects and the mandatory procedural constraints outlined in regulatory documents governing its use in clinical studies.


Interaction Scope: Pharmacodynamic Potentiation

Category Official Regulatory Documentation Entity / Finding
Medicinal product categories with documented interactions: Products with hypotensive effects (e.g., Vasodilators, Antihypertensives).
Mechanistic basis of interactions: Pharmacodynamic interaction resulting from additive systemic vasodilation.
Timing-based interaction rules (if applicable): Mandatory dose adjustment or discontinuation based on Systolic Blood Pressure (SBP) thresholds.
Interaction-related restrictions: Administration must be discontinued if SBP falls below 100 mmHg (procedural constraint from trial protocol).
Population-specific interaction notes (if applicable): The interaction outcome (hypotension) required procedural intervention in a higher percentage of Relaxin-treated patients compared to the placebo group.

Official Interaction Statements

  • Co-administration with hypotensive agents may result in an additive effect on systemic vascular resistance and blood pressure, formally documented as hypotension.
  • No formal contraindications or explicit warnings regarding interactions with CYP450 enzymes, transporters (P-gp, OATP), food, alcohol, or herbal products are documented in regulatory trial summaries.

The regulatory documents define the product's interaction structure primarily through the risk of pharmacodynamic potentiation with other hypotensive agents, necessitating specific and mandatory procedural constraints on the rate of administration. The official restrictions are solely determined by continuous monitoring of the resulting change in blood pressure.

Mechanism of Action

How Relaxin Works

The mechanism of Recombinant Human Relaxin-2 is defined by its action on a specialized membrane receptor, leading to concurrent effects on the circulatory system and connective tissue structure. The molecule operates through two key mechanistic domains to produce its core physiological changes.


⁠Activation of the RXFP1 Receptor and Vasodilation

Relaxin acts as an agonist for the Relaxin Family Peptide Receptor 1 ( RXFP1), a G protein-coupled receptor found in blood vessel walls. Activation of RXFP1 rapidly initiates the PI3K/eNOS cascade, leading to increased production of Nitric Oxide ( NO). This molecular sequence causes the relaxation of vascular smooth muscle, resulting in a direct decrease in systemic vascular resistance and increased arterial compliance.


⁠Extracellular Matrix Remodeling and Anti-Fibrotic Action

This domain focuses on the sustained action of Relaxin on tissue structure. By maintaining RXFP1 signaling, the molecule modulates gene expression in connective tissue cells (fibroblasts), actively inhibiting the pro-fibrotic TGF-beta 1 signaling axis while simultaneously promoting the activity of Matrix Metalloproteinases ( MMPs). This coordinated effect leads to a net degradation of accumulated collagen, which biologically translates to reduced tissue stiffness and structural remodeling.

Dosage and Administration Information

How Relaxin is Used: Official Administration Guidelines

The use of Recombinant Human Relaxin-2 (Serelaxin) is defined by strict procedural protocols which mandate precise delivery methods. This medicine is administered under highly controlled conditions, reflecting the critical-care context of its documented use.


Core Administration Principles

Principle Official Guideline
Route of Administration Intravenous (IV) infusion (administered directly into a vein).
Dosing Regimen A nominal, weight-adjusted dose of 30 micrograms per kilogram per day (30 mug/kg/day) is utilized.
Frequency & Duration Continuous infusion administered without interruption for a fixed duration of 48 hours (two days).

Procedural and Contextual Requirements

Relaxin is supplied as a concentrate that requires dilution prior to administration, typically using a 5% dextrose solution, and this preparation is handled by trained staff. The official procedure requires that the final solution be delivered using a continuous infusion pump over a dedicated IV line to ensure the steady delivery of the weight-adjusted dose. Due to the nature of the administration and the need for constant monitoring, the entire course of treatment must take place in an inpatient hospital setting under specialized medical supervision. The dosing schedule is calculated based on the adult patient's weight, which provides a necessary, high-level adjustment for body mass.

Recent Clinical Evidence

Research Evidence / Overview of Studies

This section describes the clinical studies that have evaluated the drug, focusing on its potential application in conditions related to fibrosis and restricted tissue function.

Key Clinical Trials

Trial 1: Assessment in Systemic Sclerosis (SSc)

This study evaluated the safety and efficacy of the drug in participants with diffuse cutaneous systemic sclerosis, a condition characterized by skin and internal organ fibrosis. The trial was a randomized, double-blind, placebo-controlled study.

  • Primary Findings: The study reported changes in skin thickening scores (e.g., modified Rodnan skin score) over the treatment period. Participants receiving the drug demonstrated a larger mean change in this measure compared to the placebo group.
  • Study Duration: The trial monitored participants over 24 weeks.

Trial 2: Research in Chronic Heart Failure (CHF)

This research examined the drug's effect on short-term hemodynamic function in participants with chronic heart failure. The study involved a controlled infusion period.

  • Primary Findings: The research reported changes in cardiac output and systemic vascular resistance across the study duration. The drug was associated with dose-related changes in these parameters.
  • Patient Population: The study population included individuals with stable, moderate-to-severe CHF.

Adverse Event and Tolerability Summary

The studies included analysis of short-term adverse event and tolerability data; information regarding long-term events is currently limited.

  • Reported Adverse Events: The most frequently reported adverse events (occurring in more than 5% of participants) included headache, mild dizziness, and flushing. These events were generally reported as mild and transient.
  • Exclusions: Studies often excluded participants with severe pulmonary hypertension or significant baseline hypotension. Research describing the data for certain patient populations is currently limited.

Key Studies & References RELAXin in Acute Heart Failure (RELAX-AHF) Trial (Teerlink et al., 2013)

Frequently Asked Questions (FAQ)

Common questions about Relaxin (FAQ)

Q: How is Relaxin different from a standard NSAID or common pain reliever?

Official information describes Relaxin as a peptide hormone that belongs to a class of medications known as vasodilators and anti-fibrotic agents. This class is fundamentally different from standard pain relievers, such as non-steroidal anti-inflammatory drugs (NSAIDs), which primarily work by reducing inflammation. Relaxin's action involves widening blood vessels and affecting tissue stiffness, rather than direct anti-inflammatory pain relief.

Q: Is there a need to gradually reduce the dose of Relaxin before stopping it?

The medicine is administered as a continuous, fixed-duration intravenous infusion, typically for 48 hours. Official data indicates that the drug's pharmacological effects decline rapidly upon cessation because the peptide has a short half-life in the body. This rapid decline is a documented safety characteristic.

Q: Are there clinical trials currently studying Relaxin for new therapeutic uses?

Research studies have evaluated the medicine for its effects in conditions such as Acute Heart Failure and Systemic Sclerosis. The development of the medicine continues to be tracked. Information on the status of ongoing clinical trials for new potential uses can typically be found in public clinical trial registries.

Q: What kind of specialist is typically the one to prescribe Relaxin?

Regulatory administration guidelines restrict the use of this medicine to an inpatient hospital setting. Treatment requires constant monitoring under the care of specialized medical supervision. This typically involves specialists in critical care or cardiology, depending on the context of the treatment.

Q: Why does Relaxin require a prescription from a healthcare professional?

As a peptide hormone in an injectable solution, the medicine requires specialized preparation and administration. It must be delivered via intravenous infusion, necessitating constant monitoring by healthcare professionals. This level of oversight ensures proper delivery and management of potential reactions.

Q: Is the effect of Relaxin on the body different for men and women?

Clinical trial data was analyzed across different adult populations. Official safety and efficacy reviews did not report any significant subgroup variation in effect based on the sex (male or female) of the patients studied.

Q: What is the purpose of the 'inactive ingredients' listed in Relaxin?

The active ingredient is a sensitive protein. The inactive ingredients, which form the aqueous base or vehicle, are included to keep the active peptide protein stable. These ingredients help ensure the product remains sterile and maintains stability for intravenous administration.

Q: Is there an antidote or reversal agent for Relaxin overdose?

Official information does not mention a specific antidote or reversal agent. However, a key safety characteristic of the drug is that its effects decline rapidly upon cessation of the infusion due to its short half-life.

Q: Does taking Relaxin affect the results of common lab tests?

Safety reviews have noted changes in certain blood tests. A decrease in markers like haemoglobin and haematocrit has been observed. This change is attributed to the effect of haemodilution, which means the blood becomes slightly more diluted.

Q: What specific signs would indicate a need to contact a healthcare provider about a side effect?

The chief safety concern is a drop in blood pressure, known as hypotension. The administration protocol establishes the Systolic Blood Pressure (SBP) threshold of 100 mmHg as the point where medical staff must initiate intervention. This threshold is the key measurement used for managing safety during administration.

Q: Is it true that the drug Relaxin could affect joints or ligaments in the body?

The documented action of the drug is classified as anti-fibrotic, which means it works against tissue stiffening. Its mechanism involves promoting the breakdown of excess collagen in connective tissues. This is the basis for its documented ability to affect tissue stiffness.

Q: Can Relaxin be taken at the same time as other prescription pain medications?

The interaction profile is primarily limited to other medicines that also cause blood pressure to drop (hypotensive agents), as this can lead to an additive effect. Official documents do not contain formal warnings or contraindications regarding interactions with non-hypotensive pain medications.

Q: Are there any over-the-counter drugs that should not be taken with Relaxin?

Official documentation does not provide explicit warnings against specific general over-the-counter drugs. Furthermore, there are no documented formal contraindications or warnings regarding food, alcohol, or herbal products.

Q: How quickly does a patient typically start noticing the effects of Relaxin?

The medicine has a rapid onset of action. Adverse reactions, such as hypotension, are typically associated with the start of the intravenous infusion. This suggests the drug's effects, including changes in blood pressure, occur very quickly once the infusion has begun.

Q: Why are there different formulations (capsule, injection) of Relaxin discussed online?

The only official form is an injectable solution for intravenous infusion. This is required because the drug is a protein and must be delivered directly into the bloodstream to avoid being degraded by the digestive system. Any discussion of a capsule form does not align with the official product information.

Q: What does "contraindicated" mean in the context of Relaxin?

The term contraindicated refers to a specific circumstance or condition that makes a treatment inappropriate because the risks outweigh any benefit. For this medicine, official regulatory reviews state that no formal contraindications are documented.

Q: What is the difference between brand-name Relaxin and its generic equivalent, if one exists?

The medicine is a specific protein known as Recombinant Human Relaxin-2 (Serelaxin). Because the drug has not received full marketing approval in major global markets, a standard generic equivalent is not available.

How should Relaxin be stored and disposed of?

Official Storage and Disposal Requirements

The storage and disposal of Relaxin (Recombinant Human Relaxin-2 injectable solution) are governed by specific regulatory requirements to maintain its stability and ensure environmental safety.

Condition Regulatory Requirement
Temperature Store refrigerated between 2, C and 8, C (36^circF and 46^circF). Do not freeze.
Protection Store in the original carton to protect the solution from light.
Child Safety Keep the medication out of the sight and reach of children.
Post-Use Discard any unused product immediately after administration (for single-dose vials).
Disposal Dispose of used needles, syringes, and vials in a designated puncture-resistant sharps container. Expired or unwanted product must be disposed of according to local pharmaceutical waste regulations, and should not be thrown into household trash or wastewater.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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