Optalidon

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Optalidon

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Method of action: Analgesic

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Medically reviewed

Marina Burgos

Last updated on 22/12/2025

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 Optalidon

Property Description
Active Ingredients Propyphenazone, Caffeine
Primary Forms Tablet (Oral), Suppository (Rectal)
Pharmacological Class Compound Analgesic, NSAID (Pyrazolone), CNS Stimulant (Methylxanthine)
General Purpose Symptomatic relief of pain and fever
Origin Fixed-dose combination of synthetic and natural/synthetic components

Optalidon is a pharmaceutical preparation defined as a Fixed-Dose Combination (FDC) compound analgesic, integrating the active ingredients Propyphenazone and Caffeine. This composition is primarily intended for the symptomatic relief of pain and fever. This medicine structurally integrates two distinct actions, placing it in the pharmacological categories of a Nonsteroidal Anti-inflammatory Drug (NSAID), specifically a pyrazolone derivative, and a Central Nervous System (CNS) Stimulant.

Optalidon: A Differentiated Analgesic Formulation

The unique profile of Optalidon is rooted in its composition, which utilizes Propyphenazone as the primary analgesic and antipyretic agent, distinguishing it from formulations relying solely on common NSAIDs. Propyphenazone belongs to the pyrazolone class of compounds.

Optalidon is available as both an oral tablet and a suppository. This provides alternative administration routes, potentially benefiting patients who may experience difficulties with swallowing oral medications. The pyrazolone structure is typically a synthetic derivative, while the methylxanthine component, Caffeine, can be either naturally derived or synthesized.

The Pharmacological Class and Dual Action

The core classification is based on the components: Propyphenazone is a pyrazolone derivative, and Caffeine is a methylxanthine derivative. Propyphenazone's pain-relieving action is associated with the inhibition of prostaglandin synthesis.

The inclusion of Caffeine serves as an analgesic adjuvant. Combining Caffeine with analgesics enhances the pain-fighting action. This dual mechanism is clinically recognized for providing symptomatic relief from acute pain, such as common headaches, while simultaneously counteracting associated fatigue. The overall design emphasizes a comprehensive approach to managing general discomfort and fever.

Regulatory References

  1. Caffeine as an analgesic adjuvant for acute pain in adults (NIH/PMC)

What side effects are possible with Optalidon?

Possible Side Effects and Safety Information

Adverse reactions associated with this fixed-dose combination (Propyphenazone/Caffeine) are classified by regulatory authorities based on the affected organ system and frequency of occurrence. The profile reflects the properties of a pyrazolone NSAID and a central nervous system stimulant.

Adverse Reaction Scope

Side effects documented in regulatory labeling primarily involve the Gastrointestinal System (e.g., nausea, stomach pain, irritation) and the Nervous System (e.g., dizziness, difficulty sleeping, restlessness), which are generally classified as uncommon or occasional.

  • Dermatological Reactions: Skin rash, redness (erythema), and itching (pruritus) are known adverse effects.
  • Cardiac Effects: Due to the caffeine component, palpitations or an increased heart rate are listed in the safety profile.

Serious Adverse Reactions and Systemic Risk

Of critical note is the risk associated with the pyrazolone component, Propyphenazone, which can rarely cause severe Blood and Lymphatic System Disorders. The most serious, very rare risk documented in regulatory sources is Agranulocytosis, a significant reduction in white blood cells. Additionally, the label notes isolated reports of severe hypersensitivity reactions, including the possibility of anaphylactic shock.

Safety Constraints and Special Populations

Official regulatory documents stipulate specific limitations and contraindications for Optalidon use:

  • Contraindications: The medicine is restricted or contraindicated in individuals with known hypersensitivity to pyrazolone derivatives or caffeine, pre-existing blood disorders, active gastrointestinal ulcers or bleeding, and severe hepatic (liver) or renal (kidney) impairment.
  • Population Limits: Use is generally not recommended for children under 12 years of age or during pregnancy and lactation, due to the risks associated with both the NSAID and caffeine components.
  • Exposure Note: Regulatory texts caution against exceeding the maximum recommended dose and advise against prolonged use without medical oversight, as this can increase the risk of severe adverse events.
  • Caffeine Restriction: To prevent exaggerated stimulant effects, the label advises avoiding the simultaneous consumption of high amounts of caffeine from other dietary sources.

Overdose and Emergency Response

Overdose and When to Seek Help

An overdose of Optalidon, a fixed-dose combination of Propyphenazone and Caffeine, is associated with a specific dual-component toxicity profile that mandates immediate medical intervention. The officially documented clinical manifestations affect multiple physiological systems, as described in regulatory documents.

Documented signs often include gastrointestinal effects such as nausea, vomiting, and abdominal pain. Central Nervous System effects range from agitation, tremor, confusion, and drowsiness to severe manifestations like seizures and coma. Cardiovascular effects are documented as tachycardia and palpitations, which can progress to life-threatening cardiac arrhythmias.

Regulators mandate that individuals must seek immediate medical attention or contact emergency services immediately upon any suspicion of overdose or accidental ingestion. The recognized risk of severe outcomes, including metabolic acidosis and potential acute hepatic or renal injury, necessitates urgent assessment.

Management protocols, as described in official prescribing information, focus on symptomatic and supportive treatment since no specific antidote is known for the combination. Recommended measures include gastric decontamination procedures, such as administering activated charcoal. Hospital monitoring is required, specifically including continuous ECG surveillance and monitoring of vital signs, fluid and electrolyte balance, and organ function. Official documentation notes that pediatric patients and those with pre-existing hepatic or renal impairment may face increased severity and require cautious management.

Therapeutic Uses of Optalidon

What Optalidon Treats: Main Uses and Benefits

The therapeutic goal of this fixed-dose combination is to provide supportive relief across therapeutic domains where additional symptomatic support is needed, intended for supportive analgesic action.

This medicine is commonly used across conditions characterized by episodic symptom patterns, may assist in easing the symptoms associated with primary headache disorder, localized dental pain, and recurrent menstrual discomfort (dysmenorrhea). It is also applied in settings marked by temporary physiological imbalance, addressing generalized muscle aches, joint pain of mild to moderate intensity, and elevated body temperature.

In these acute, challenging episodes, the compound is applied in scenarios where additional management of discomfort is required, supporting general well-being during symptomatic phases. As one core principle of its use highlights:

“The formulation is relevant for easing symptoms related to systemic imbalance, including antipyretic support, and plays a role in managing physical discomfort.”

In situations where symptoms related to physical discomfort or systemic imbalance become temporarily overwhelming, the medicine may assist with managing symptoms that interfere with daily comfort.

Quick Fact: Relief for Acute Discomfort
Relevant for: Pain and fever associated with acute or disruptive episodes.
Primary Benefit: Supports the patient during difficult episodes by easing distress, including associated fatigue.

Eligibility and Restrictions for Use

Who Can and Cannot Use Optalidon?

This section details the official regulatory population eligibility rules for Optalidon (Propyphenazone/Caffeine).

Eligibility Scope Status
Approved Age Group Adults and Adolescents (12+ years)
Pediatric Use (<12 yrs) Contraindicated / Not Recommended
Pregnancy and Lactation Contraindicated

Use is absolutely contraindicated for individuals with known hypersensitivity to the active ingredients, other pyrazolone derivatives, or other NSAIDs (including aspirin). Non-eligibility also applies to severe disorders, specifically: granulocytopenia, acute hepatic porphyria, G6PD deficiency, and severe hepatic, renal, or cardiac insufficiency. Individuals with pre-existing anxiety disorders must also avoid use.

The medicine requires caution and restricted use for populations with moderate hepatic or renal impairment, pre-existing hypertension, a history of peptic ulcer/GI bleeding, or conditions like asthma. Older adults are advised to use the lowest effective dose.

What should I know about interactions with other medicines?

The interaction profile of Optalidon (Propyphenazone/Caffeine) is officially documented by regulatory authorities based on the combined pharmacological effects of its active components.

Documented Pharmacodynamic and Substance Interactions

Co-administration with Anticoagulants (e.g., Warfarin) is associated with an increased risk of bleeding due to the Propyphenazone component’s classification as a Nonsteroidal Anti-inflammatory Drug (NSAID). Official regulatory warnings also advise against the use of Optalidon with other NSAIDs due to the additive pharmacological risk of severe gastrointestinal adverse effects.

Interactions with Alcohol (Ethanol) and Other Caffeine-Containing Products (foods, beverages, supplements) are subject to regulatory caution. These restrictions address the risk of cumulative central nervous system (CNS) effects or potential masking of CNS impairment when combined with the active Caffeine component.

Pharmacokinetic and Exposure Constraints

Regulatory documentation outlines that certain medicines can modify the plasma exposure of Optalidon's components via metabolic pathways:

  • Decreased Exposure: Strong CYP Enzyme Inducers (e.g., Rifampin, Phenytoin) may accelerate the hepatic metabolism of the Propyphenazone component, leading to decreased plasma concentrations.
  • Increased Exposure: Strong CYP1A2 Inhibitors (e.g., Fluvoxamine) are documented to reduce the clearance of the Caffeine component, resulting in increased systemic exposure. Chloramphenicol may similarly increase the exposure of the Propyphenazone component by inhibiting its metabolism.

Use with Phenobarbital is specifically cautioned against or contraindicated in certain populations, reflecting a drug-drug interaction risk related to the Caffeine component.

Mechanism of Action

Modulating Prostaglandin Synthesis and Nociceptive Signaling

The core mechanism involves the Propyphenazone component acting as a competitive inhibitor of the Cyclooxygenase (COX-1 and COX-2) enzymes. This action is a key regulatory step within the Arachidonic Acid Cascade, leading to a reduction in the synthesis of prostaglandins—chemical mediators that sensitize peripheral pain-sensing neurons and reset the body's thermoregulatory set-point. This mechanism is applied to adjust pathway activity that escalates under certain conditions, contributing to the dampening of peripheral nociceptive signaling and the modulation of the hypothalamic thermal set-point.

Antagonizing Central Adenosinergic Inhibition

The Caffeine component engages a separate pathway by acting as a competitive antagonist primarily at the Adenosine Receptors ( A1 and A2 A subtypes). Blocking these inhibitory receptors removes a natural brake on certain central nervous system (CNS) activity, leading to increased neuronal firing and the release of excitatory neurotransmitters. This targeted pathway adjustment supports the regulation of processes driven by distinct signaling patterns, leading to disinhibition of central nervous system activity, which affects catecholamine release, and an alteration of local cerebrovascular tone.

Dosage and Administration Information

The use of Optalidon, a Fixed-Dose Combination (FDC) analgesic, is governed by specifications detailed in prescribing information. These instructions define the proper administration route, dosing limits, frequency, and duration of use.

Administration Parameters

Parameter Standard Instruction
Routes of Administration The medicine is approved for systemic use via the oral route (tablets) and may be available as a rectal suppository.
Standard Adult Dose The standard single dose for adults is 1 to 2 tablets. Subsequent single doses may be administered as needed for symptomatic relief.
Dosing Frequency and Maximum Dosing should not be repeated more frequently than every 4 hours. The total daily intake must not exceed 6 tablets over any 24-hour period.
Administration Conditions Oral tablets should be taken with ample water or other fluid. Oral use is often instructed to occur 1 to 2 hours after a meal. Tablets must be swallowed whole.
Course Duration Restriction The treatment course is limited to short-term use. Use for fever should not exceed 3 consecutive days, and use for pain relief should not exceed 5 to 7 days without consultation.

Population-Specific Rules

Administration rules specify adjustments for certain age groups and populations:

  • Adolescents (12–16 years): The single dose is reduced to 1 tablet, with frequency limits applying as for adults.
  • Children Under 12: The use of this combination is not recommended for children under 12 years of age.
  • Renal Impairment: For patients with moderate kidney impairment, the minimum required interval between doses is extended to at least 8 hours to allow for proper clearance of components.

The use protocol mandates strict adherence to these limits. These instructions define how much and how often the medication is used across all approved formulations.

Recent Clinical Evidence

Research evidence / Overview of studies for Optalidon

Evidence from Studies on Pain and Fever Relief

The research on Optalidon involves studies on its components, Propyphenazone and Caffeine, which have been evaluated for outcomes related to physical discomfort and systemic imbalance, such as fever. Research explored the antipyretic properties of Propyphenazone and monitored the combination with other analgesics, where data show patterns related to differences in the measured outcomes related to physical discomfort; the component was studied for its role as an analgesic adjuvant. The evidence level for this general effect is currently categorized as Moderate. However, certainty remains low regarding the specific fixed-dose combination (FDC) when compared to the broader evidence landscape for some other analgesic compounds, as follow-up durations were limited to the acute phase.

Research Findings for Acute Episodic Conditions and Combined Action

Research examined conditions characterized by fluctuating or episodic manifestations, including primary headache disorder, dental pain, muscle aches, joint pain of mild to moderate intensity, and recurrent menstrual discomfort (dysmenorrhea). These studies monitored patient-reported outcomes describing perceived discomfort. For specific indications like headache, evidence is limited to studies supporting the general class of analgesics and the concept of Caffeine as an adjuvant. Studies also explored how the Propyphenazone and Caffeine combination was studied for its supportive analgesic action and monitored outcomes related to associated fatigue.

Limitations and Research Gaps

While the existing evidence primarily focuses on short-term relief, long-term effects are not fully established. Follow-up durations were limited, and there is limited information for long-term outcomes. This area, where data are still emerging, is considered a research gap. Furthermore, data for certain groups remain insufficient as the studies primarily explored general adult populations, meaning that results apply only to the populations studied. Comparative evidence is lacking for the Optalidon FDC against some common single-ingredient pain relievers, and data for certain groups remain insufficient.

Key Studies & References

  1. Caffeine for headache and pain relief in adults (Cochrane Review)

Frequently Asked Questions (FAQ)

Common questions about Optalidon (FAQ)

Q: Is Optalidon considered a strong pain reliever?

Official drug labels and studies for combination analgesics containing Propyphenazone generally indicate use for the relief of mild to moderate pain of various origins. The combination formulation is described as providing effective relief for discomfort within this intensity range, leveraging the combined effects of its active ingredients.

Q: Can I take Optalidon if I am also taking antidepressants?

Information in regulatory documents notes that certain antidepressants may affect the metabolism of components in combination analgesics. Furthermore, the Caffeine component is a central nervous system (CNS) stimulant, and there is a potential for cumulative CNS effects when used with certain other psychoactive medicines. Patients are generally directed to consult the official package information for specific known interactions.

Q: Can Optalidon be taken on an empty stomach?

Regulatory guidance often states that this medication should be taken with water. While some documents state it can be taken with or without food, taking it after a meal may help reduce the risk of gastrointestinal irritation. This caution is typically advised due to the presence of the Nonsteroidal Anti-inflammatory Drug (NSAID) component.

Q: Is it possible to become dependent on Optalidon with long-term use?

The official duration of treatment for Optalidon is restricted to short-term use (e.g., 5 to 7 days for pain). This restriction is in place to minimize the risk of drug abuse or physical dependence, which is associated with the prolonged or excessive use of certain combination analgesics.

Q: Is there any risk of rebound headache with Optalidon, according to official information?

Yes, the product's duration of use is explicitly limited to short-term periods. This limitation reflects the documented risk of developing Medication-Overuse Headache (MOH), commonly known as a rebound headache, which can occur with frequent or prolonged use of combination pain relievers containing caffeine and analgesics.

Q: What is the main role of each active component in Optalidon?

Propyphenazone acts as the main analgesic (pain reliever) and antipyretic (fever reducer). The second component, Caffeine, is included as an analgesic adjuvant, which means its role is to enhance or support the pain-relieving effect of the primary analgesic component.

Q: What research evidence supports the use of Optalidon for its approved purpose?

Research cited in regulatory documents supports the combination's overall efficacy for pain relief. This is largely based on the Propyphenazone component's fast onset of action and the finding that Caffeine is recognized for its ability to enhance the pain-fighting action of analgesics, leading to effective symptomatic relief.

Q: Why is Optalidon sometimes used instead of common over-the-counter medicines?

Optalidon is defined as a Fixed-Dose Combination (FDC) that integrates the action of an NSAID (Propyphenazone) and a CNS stimulant (Caffeine). Regulatory documents describe the combination as integrating the actions of two components, a rationale supported by research examining its use in acute pain relief.

Q: How quickly do people usually feel the effects of Optalidon?

Regulatory documents note that Propyphenazone, the main analgesic component, has a proven fast onset of action. Symptomatic relief is typically noted to occur within 30 to 60 minutes after taking a dose.

Q: What is the average duration of action for Optalidon?

The official dosing frequency provides an indication of the expected duration of action. Doses are typically not recommended to be repeated more frequently than every 4 hours, suggesting the pain-relieving effect lasts up to that time.

Q: Does Optalidon contain caffeine?

Yes, Optalidon is a combination analgesic that contains Caffeine as one of its active pharmaceutical ingredients. The Caffeine component is included as an adjuvant to help support the overall pain-relieving effects.

Q: How does Optalidon relate to other pain medications that contain similar ingredients?

Optalidon belongs to the class of Fixed-Dose Combination (FDC) analgesics that pair a pain reliever with caffeine. While other combination products may use different primary analgesics, the principle of combining an analgesic with caffeine to support effectiveness is a recognized approach across regulatory documents.

Q: Is Optalidon the same as Optalgin or other similar sounding drug names?

No. Optalidon contains Propyphenazone and Caffeine. Optalgin is a brand name for a different analgesic drug called Metamizole (Dipyrone). Although both belong to the pyrazolone class and share similar risks, they are chemically distinct and should not be confused.

Q: What is the difference between Optalidon and standard paracetamol (acetaminophen)?

Optalidon's primary analgesic component is Propyphenazone, which is classified as a Nonsteroidal Anti-inflammatory Drug (NSAID). Standard paracetamol (acetaminophen) is a chemically different pain reliever that is generally not classified as an NSAID and lacks the anti-inflammatory properties associated with NSAIDs like Propyphenazone.

Q: Can Optalidon be used for tension headaches?

Official indications for this class of combination analgesic commonly include the relief of mild to moderate pain, such as headache and migraine. This covers the symptoms and discomfort associated with a tension-type headache.

Q: Is Optalidon effective for muscle pain or only headaches?

The therapeutic indications documented in regulatory texts for this combination are broad and include relief for various types of discomfort. Approved uses commonly extend beyond headaches to include relief for joint pain and muscle aches (myalgia).

Q: Are there any food or drinks that should be avoided when using Optalidon?

The official product information advises against the co-administration of alcohol. Caution is also advised regarding the simultaneous consumption of high caffeine-containing products (including certain foods, beverages, or supplements) to prevent potential cumulative stimulant effects.

Q: Does Optalidon interact with herbal supplements?

While specific herbal products may not be fully detailed, the Propyphenazone component is an NSAID. Caution is generally advised with any herbal product known to increase the risk of bleeding or hemorrhage (for example, Ginkgo Biloba), due to the known interaction warnings with blood thinners.

Q: Why do some people experience mild dizziness after taking Optalidon?

Dizziness is listed in regulatory documents as an occasional side effect involving the Nervous System. This can be associated with the pharmacological action of the pyrazolone component or the central nervous system stimulant effect of the Caffeine component.

Q: What should be done if a potential drug interaction with Optalidon is suspected?

If a potential drug interaction or new, severe symptoms are suspected, official public health guidance recommends that the individual immediately contact a healthcare professional or emergency services for assessment and guidance.

Q: What is the current legal status of Optalidon in major countries?

The regulatory status of this combination is variable depending on the country. While it is available as an over-the-counter (OTC) drug in some regions, it is classified as a prescription-only medication in others. In a few countries, its use has been restricted due to safety concerns.

Q: Does Optalidon show up on a standard drug screening test?

The components of Optalidon (Propyphenazone and Caffeine) are distinct chemical compounds. They can be detected and identified using standard analytical toxicology methods, such as chromatography and mass spectrometry, in biological samples when a screening test is specifically looking for them.

Q: Why is Optalidon sometimes restricted to prescription-only status?

The restriction to prescription-only status in certain regions is primarily due to the rare but serious risk of blood and lymphatic system disorders. Regulatory warnings specifically point to the risk of agranulocytosis associated with the Propyphenazone (pyrazolone) component.

Q: Can Optalidon be used for chronic pain management, as per official guidance?

No. Official regulatory instructions explicitly limit the use of this product to short-term relief (e.g., 5 to 7 days for pain). It is not approved or recommended for the long-term management of chronic pain.

How should Optalidon be stored and disposed of?

How to Store and Dispose of Optalidon

The storage and disposal of this medicine must comply strictly with the conditions defined in official regulatory labeling to ensure product stability and safety.

Storage Requirements

Condition Regulatory Requirement
Temperature Store at room temperature, typically not above 30°C.
Protection Must be protected from light and moisture; store in the original, tightly closed package.
Handling Do not freeze the medicinal product.
Child Safety Keep out of the sight and reach of children.

Disposal Instructions

Disposal of unused or expired Optalidon must follow labeled instructions or local regulatory requirements. The preferred method is using a drug take-back program. If no take-back option is available, the product should be mixed with an undesirable substance (e.g., dirt, coffee grounds) in a sealed container before being placed in household trash. The product must not be thrown into wastewater or sewage.

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

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