DAFLON 1000MG

Indications

• Cardiovascular diseases
• Cancer prevention and treatment
• Inflammatory conditions
• Allergic disorders
• Neurodegenerative diseases

Dosage

Children: Paediatric dosing is not well established and may vary based on the specific flavonoid.

Adults: Dosage varies widely depending on the specific flavonoid compound and the condition being treated. Refer to specific product information for guidance.

Mechanism of action

Flavonoids exert their biological effects primarily through their ability to modulate cell signaling pathways, influencing gene expression and enzyme activity. They act as antioxidants, scavenging free radicals and reducing oxidative stress. Additionally, flavonoids can affect the activity of various enzymes, such as cyclooxygenases and lipoxygenases, which are involved in inflammatory processes. They may also enhance endothelial function and modulate vascular tone, contributing to their cardioprotective benefits.

Pharmacodynamics

Flavonoids demonstrate a wide range of pharmacodynamic effects, including anti-inflammatory, anti-cancer, and neuroprotective activities. They can inhibit the proliferation of cancer cells, induce apoptosis, and prevent metastasis. In the cardiovascular system, flavonoids help improve endothelial function, reduce blood pressure, and lower LDL cholesterol levels. Their antioxidant properties contribute to the protection of cells from oxidative damage, which is implicated in various chronic diseases.

Pharmacokinetics

Flavonoids are absorbed from the gastrointestinal tract, with bioavailability varying significantly among different flavonoids due to factors such as solubility and metabolism. They undergo extensive metabolism in the liver and intestines, leading to the formation of various metabolites. The elimination half-life of flavonoids can range from hours to days, depending on the specific compound and individual metabolism. Flavonoids are primarily excreted in urine, often as conjugated metabolites.

Pregnancy

Flavonoids are generally considered safe during pregnancy; however, specific products should be evaluated for safety.

Breast-feeding

Flavonoids are generally considered safe during breastfeeding; however, specific products should be evaluated for safety.

Storage

Store in a cool, dry place away from light.

Indications

• Schizophrenia
• Psychotic disorders
• Severe anxiety and agitation
• Nausea and vomiting
• Intractable hiccups

Dosage

Adults: The usual starting dose for adults is 25 mg to 50 mg taken orally, which can be increased gradually to achieve the

Mechanism of action

Chlorpromazine acts as an antagonist on multiple postsynaptic receptors, including dopaminergic receptors (D1, D2, D3, D4), serotonergic receptors (5-HT1, 5-HT2), histaminergic receptors (H1), alpha-adrenergic receptors (alpha1, alpha2), and muscarinic receptors (M1, M2). This blockade leads to reduced dopaminergic activity, which alleviates psychotic symptoms, while the interaction with serotonergic and histaminergic receptors contributes to its anxiolytic, sedative, and antiemetic effects. Additionally, it has a weak presynaptic inhibitory effect on dopamine reuptake, providing mild antidepressive and antiparkinsonian effects.

Pharmacodynamics

Chlorpromazine primarily exhibits its effects at subcortical levels of the central nervous system. It is recognized for its strong antiadrenergic effects and weaker peripheral anticholinergic activity. The drug also shows slight antihistaminic and antiserotonin activity, contributing to its broad spectrum of effects on mood, behavior, and various physiological functions.

Pharmacokinetics

Chlorpromazine is well-absorbed following oral administration and is extensively metabolized in the liver. The drug's half-life varies significantly among individuals, typically ranging from 30 to 50 hours, but can be longer in some patients. It is primarily excreted in the urine as metabolites, with minimal unchanged drug being eliminated. The pharmacokinetics of chlorpromazine may be influenced by factors such as age, liver function, and concurrent medications.

Contra-indications

• Hypersensitivity to chlorpromazine or any of its components
• Comatose states
• Severe central nervous system depression
• Bone marrow depression
• Porphyria
• Severe liver dysfunction
• Pheochromocytoma

Adverse effects

• Sedation
• Weight gain
• Orthostatic hypotension
• Extrapyramidal symptoms
• Dry mouth
• Blurred vision
• Constipation
• Urinary retention
• Tachycardia
• Sexual dysfunction
• Akathisia
• Neuroleptic malignant syndrome

Interactions

• CNS depressants (e.g., alcohol, benzodiazepines) may enhance sedative effects
• Antihypertensive agents may have additive hypotensive effects
• Anticholinergic drugs may exacerbate anticholinergic effects
• Dopamine agonists may have reduced efficacy

Precautions

• Use with caution in patients with a history of seizures
• Monitor for signs of tardive dyskinesia
• Use cautiously in elderly patients, particularly those with dementia-related psychosis
• Regular monitoring of blood pressure is advised
• Consider the risk of metabolic syndrome

Pregnancy

Chlorpromazine should only be used in pregnancy if the potential benefit justifies the potential risk to the fetus. It is categorized as a pregnancy category C drug.

Breast-feeding

Chlorpromazine is excreted in breast milk. Caution should be exercised when administering to nursing mothers.

Storage

Store in a cool, dry place away from light. Keep out of reach of children.

Formulations

• Tablets (various strengths)
• Oral solution
• Injectable solution

Dosage

Children: Refer to specific drug monographs for dosing information, as dosing varies by the active ingredient and therapeutic indication.

Adults: Refer to specific drug monographs for dosing information, as dosing varies by the active ingredient and therapeutic indication.

Mechanism of action

Micronisation itself does not alter the inherent mechanism of action of a drug, but it improves the drug's solubility and absorption characteristics. For drugs that are micronised, the enhanced surface area allows for more rapid dissolution in the gastrointestinal tract, which can lead to increased plasma concentrations and improved therapeutic effects.

Pharmacodynamics

The pharmacodynamics of micronised drugs depend on the specific active pharmaceutical ingredient (API) being micronised. Generally, micronisation enhances the bioavailability of drugs that exhibit poor solubility, leading to more effective pharmacological responses at lower doses. This may result in a reduction in side effects and improved patient compliance.

Pharmacokinetics

Micronised drugs typically exhibit altered pharmacokinetic profiles compared to their non-micronised counterparts. The increased surface area and improved solubility facilitate quicker absorption, often resulting in higher peak plasma concentrations and potentially shorter time to peak effect. However, the elimination half-life may remain unchanged, depending on the drug's metabolism and excretion mechanisms.

Adverse effects

• Headache
• Nausea
• Dizziness
• Fatigue
• Gastrointestinal disturbances

Precautions

• Use with caution in patients with a history of hypersensitivity to the drug or its components.
• Monitor for potential allergic reactions.

Pregnancy

Safety during pregnancy has not been established. Use only if clearly needed and after evaluating risks versus benefits.

Breast-feeding

Consult a healthcare provider before use, as it is not known whether the drug is excreted in breast milk.

Storage

Store in a cool, dry place away from direct sunlight. Keep out of reach of children.

Formulations

• Micronised powder for oral administration
• Micronised capsules

Dosage

Children: Refer to specific drug formulations and product labels as purified substances can vary widely in their use and dosing.

Adults: Refer to specific drug formulations and product labels as purified substances can vary widely in their use and dosing.

Mechanism of action

The mechanism of action for purified compounds varies widely depending on the specific substance. Generally, purified drugs exert their effects by interacting with specific biological targets, such as receptors, enzymes, or ion channels, leading to a desired therapeutic effect. This interaction can involve binding to receptors to activate or inhibit signaling pathways, modulating enzymatic activity, or altering physiological processes.

Pharmacodynamics

Pharmacodynamics describes the effects of a drug on the body and the relationship between drug concentration and effect. For purified drugs, this can involve dose-response relationships and the time course of their action. The purified form often enhances potency and reduces variability in response among patients, which can lead to more predictable therapeutic outcomes. The overall effect is determined by the drug's affinity for its target, the efficacy of the drug-receptor interaction, and the downstream signaling pathways activated as a result of this interaction.

Pharmacokinetics

Pharmacokinetics involves the absorption, distribution, metabolism, and excretion (ADME) of a drug. For purified substances, absorption can be more efficient due to the absence of impurities that may affect solubility or stability. Distribution may also be enhanced, leading to higher bioavailability. Metabolism can be influenced by the structure of the purified compound, as it may be metabolized more readily by liver enzymes. Excretion typically occurs through the kidneys or liver, depending on the molecular characteristics of the purified drug.

Pregnancy

Consult with a healthcare professional, as the safety of purified forms of medications during pregnancy may vary depending on the specific substance.

Breast-feeding

Consult with a healthcare professional, as the safety of purified forms of medications during breastfeeding may vary depending on the specific substance.

Storage

Store in a cool, dry place, away from light and moisture, and keep out of reach of children.

Mechanism of action

Chlorpromazine acts as an antagonist (blocking agent) on different postsysnaptic receptors -on dopaminergic-receptors (subtypes D1, D2, D3 and D4 - different antipsychotic properties on productive and unproductive symptoms), on serotonergic-receptors (5-HT1 and 5-HT2, with anxiolytic, antidepressive and antiaggressive properties as well as an attenuation of extrapypramidal side-effects, but also leading to weight gain, fall in blood pressure, sedation and ejaculation difficulties), on histaminergic-receptors (H1-receptors, sedation, antiemesis, vertigo, fall in blood pressure and weight gain), alpha1/alpha2-receptors (antisympathomimetic properties, lowering of blood pressure, reflex tachycardia, vertigo, sedation, hypersalivation and incontinence as well as sexual dysfunction, but may also attenuate pseudoparkinsonism - controversial) and finally on muscarinic (cholinergic) M1/M2-receptors (causing anticholinergic symptoms like dry mouth, blurred vision, obstipation, difficulty/inability to urinate, sinus tachycardia, ECG-changes and loss of memory, but the anticholinergic action may attenuate extrapyramidal side-effects). Additionally, Chlorpromazine is a weak presynaptic inhibitor of Dopamine reuptake, which may lead to (mild) antidepressive and antiparkinsonian effects. This action could also account for psychomotor agitation and amplification of psychosis (very rarely noted in clinical use). The principal pharmacologic effects of chlorpromazine are similar to those of other propylamino derivatives of phenothiazine. Chlorpromazine has strong anticholinergic and sedative effects and moderate extrapyramidal effects. Chlorpromazine has strong antiemetic and adrenergic blocking activity and weak ganglionic blocking, antihistaminic, and antiserotonergic activity. The development of phenothiazine derivatives as psychopharmacologic agents resulted from the observation that certain phenothiazine antihistaminic compounds produced sedation. In an attempt to enhance the sedative effects of these drugs, promethazine and chlorpromazine were synthesized. Chlorpromazine is the pharmacologic prototype of the phenothiazines. The pharmacology of phenothiazines is complex, and because of their actions on the central and autonomic nervous systems, the drugs affect many different sites in the body. Although the actions of the various phenothiazines are generally similar, these drugs differ both quantitatively and qualitatively in the extent to which they produce specific pharmacologic effects. /Phenothiazine General Statement/ In the CNS, phenothiazines act principally at the subcortical levels of the reticular formation, limbic system, and hypothalamus. Phenothiazines generally do not produce substantial cortical depression; however, there is minimal information on the specific effects of phenothiazines at the cortical level. Phenothiazines also act in the basal ganglia, exhibiting extrapyramidal effects. The precise mechanism(s) of action, including antipsychotic action, of phenothiazines has not been determined, but may be principally related to antidopaminergic effects of the drugs. There is evidence to indicate that phenothiazines antagonize dopamine-mediated neurotransmission at the synapses. There is also some evidence that phenothiazines may block postsynaptic dopamine receptor sites. However, it has not been determined whether the antipsychotic effect of the drugs is causally related to their antidopaminergic effects. Phenothiazines also have peripheral and/or central antagonistic activity against alpha-adrenergic, serotonergic, histaminic (H1-receptors), and muscarinic receptors. Phenothiazines also have some adrenergic activity, since they block the reuptake of monoamines at the presynaptic neuronal membrane, which tends to enhance neurotransmission. The effects of phenothiazines on the autonomic nervous system are complex and unpredictable because the drugs exhibit varying degrees of alpha-adrenergic blocking, muscarinic blocking,

Pharmacodynamics

Chlorpromazine is a psychotropic agent indicated for the treatment of schizophrenia. It also exerts sedative and antiemetic activity. Chlorpromazine has actions at all levels of the central nervous system-primarily at subcortical levels-as well as on multiple organ systems. Chlorpromazine has strong antiadrenergic and weaker peripheral anticholinergic activity; ganglionic blocking action is relatively slight. It also possesses slight antihistaminic and antiserotonin activity.