K-VITA PLUS​ ​SYRUP

Indications

• Allergic conditions
• Hay fever
• Urticaria
• Pruritus
• Appetite stimulation

Dosage

Children: For children aged 6 months to 5 years, the dose is 5-15 mg daily in divided doses, adjusted according to weight, with a maximum of 2 mg/kg per day. For children aged 6-17 years weighing up to 40 kg, the initial dose is 15-25 mg daily in divided doses, adjusted as necessary to a maximum of 2 mg/kg per day. For those weighing 40 kg and above, the initial dose is 15-25 mg daily in divided doses, increased if necessary to 50-100 mg daily.

Adults: Initially, 25 mg daily, taken at night; may be increased if necessary to 25 mg 3-4 times a day. Maximum dose is 32 mg per day.

Mechanism of action

Cyproheptadine acts as a competitive antagonist at histamine H1 receptors, thereby inhibiting the action of histamine, which is responsible for allergic symptoms. Additionally, it may also block serotonin receptors, contributing to its appetite-stimulating effects.

Pharmacodynamics

The drug exhibits sedative effects by crossing the blood-brain barrier, leading to central nervous system depression. It can also produce anticholinergic effects, such as dry mouth and urinary retention, due to its action on muscarinic receptors. The sedative properties can impair the performance of skilled tasks and may be potentiated by alcohol consumption.

Pharmacokinetics

Cyproheptadine is well-absorbed from the gastrointestinal tract and undergoes hepatic metabolism. Its elimination half-life is approximately 8-12 hours, and it is excreted primarily in urine. The onset of action is typically within 1-2 hours, with effects lasting for several hours.

Contra-indications

• Acute porphyrias
• Prolonged QT-interval
• Risk factors for QT prolongation

Adverse effects

• Drowsiness
• Dizziness
• Dry mouth
• Nausea
• Constipation
• Headache
• Palpitations
• Tachycardia
• Fatigue
• Irritability
• Paradoxical excitability
• Tremor

Interactions

• Antihistamines
• Sedating agents
• Alcohol

Precautions

• Use with caution in the elderly
• Patients with epilepsy
• Prostatic hypertrophy
• Pyloroduodenal obstruction
• Susceptibility to angle-closure glaucoma
• Urinary retention

Pregnancy

Most manufacturers of antihistamines advise avoiding their use during pregnancy; however, there is no evidence of teratogenicity. Use in the latter part of the third trimester may cause adverse effects in neonates.

Breast-feeding

Most antihistamines are present in breast milk in varying amounts; although not known to be harmful, most manufacturers advise avoiding their use in mothers who are breastfeeding.

Storage

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

Formulations

• Oral suspension
• Tablets (4 mg)

Indications

• Allergic rhinitis
• Allergic conjunctivitis
• Urticaria
• Angioedema
• Anaphylaxis (as adjunct therapy)
• Appetite stimulation in certain conditions

Dosage

Children: Refer to BNF for Children for appropriate pediatric dosing, as it varies by age and condition. Generally, doses may start at 0.25 mg/kg for younger children, but specific guidelines should be

Adults: The usual adult dose for allergic conditions is 4 mg three times daily, which may be increased to a maximum of 12 mg per day as needed. For appetite stimulation, the starting dose is often 4 mg taken once or twice daily.

Mechanism of action

Cyproheptadine exerts its effects by competing with free histamine and serotonin for binding at their respective receptors. Its action as an H1 blocker is complemented by its antagonism of serotonin at 5-HT2A receptors, particularly influencing the appetite center in the hypothalamus. This dual action accounts for its appetite-stimulating properties and mitigates several pharmacodynamic effects of serotonin.

Pharmacodynamics

Cyproheptadine antagonizes several effects of serotonin and histamine, including bronchoconstriction and vasodepression. Its efficacy in combatting histamine-mediated effects has been established, although the details regarding its role in preventing anaphylactic shock remain unclear, likely linked to its anti-serotonergic activity. The drug's sedative properties arise from its central nervous system effects.

Pharmacokinetics

Cyproheptadine is well-absorbed after oral administration. It is metabolized in the liver, with a variable half-life and is primarily excreted in urine. The onset of action typically occurs within one to two hours, and the duration of action can last up to 12 hours. The pharmacokinetic profile may be influenced by individual metabolic variations.

Adverse effects

• Drowsiness
• Dizziness
• Dry mouth
• Constipation
• Blurred vision
• Increased appetite

Interactions

• cyproheptadine+metyrapone: Severe (decreases effects)
• cyproheptadine+fenfluramine: Unknown (decreases efficacy)

Precautions

• Caution in patients with glaucoma
• Caution in patients with prostate hypertrophy
• Use with caution in elderly patients due to increased sensitivity

Pregnancy

Cyproheptadine should only be used during pregnancy if the potential benefit justifies the potential risk to the fetus. Limited data are available on its safety.

Breast-feeding

Cyproheptadine is excreted in breast milk. Caution is advised when administered to breastfeeding mothers.

Storage

Store at room temperature, away from moisture and heat. Keep out of reach of children.

Formulations

• Tablets
• Syrup

Indications

• Topical treatment of skin wounds
• Moisturizing dry skin
• Management of minor burns
• Soothing irritations and inflammation of the skin

Dosage

Children: Refer to the BNF for Children for specific dosing

Adults: Apply to the affected area as needed, following the specific product instructions.

Mechanism of action

Dexpanthenol is enzymatically converted to pantothenic acid, which is integral to the formation of coenzyme A. This coenzyme acts as a cofactor in numerous enzymatic reactions, particularly those related to protein metabolism in epithelial tissues. The topical application of dexpanthenol promotes fibroblast proliferation and accelerates wound healing through enhanced re-epithelialization. It also increases the availability of coenzyme A for acetylcholine synthesis, which can enhance intestinal motility by improving peristalsis.

Pharmacodynamics

Dexpanthenol, through its conversion to pantothenic acid, plays a vital role in the synthesis of coenzyme A, which is necessary for various metabolic processes, including the transfer of acetyl groups. It directly influences the production of acetylcholine, the neurotransmitter responsible for parasympathetic nervous system functions, which include maintaining normal intestinal activity. A deficiency in acetylcholine can lead to reduced peristalsis and conditions such as adynamic ileus.

Pharmacokinetics

Dexpanthenol is well absorbed when applied topically. It penetrates the skin effectively, reaching the underlying tissues where it can exert its biological effects. The metabolism of dexpanthenol involves its conversion to pantothenic acid, which further participates in the synthesis of coenzyme A. The elimination half-life and extent of systemic absorption vary based on the formulation and route of administration, but topical use typically results in low systemic exposure.

Adverse effects

• Skin irritation
• Allergic reactions

Precautions

• Use with caution in patients with known allergies to dexpanthenol or related compounds.

Pregnancy

Dexpanthenol is generally considered safe for use during pregnancy, but it is advisable to consult a healthcare provider before use.

Breast-feeding

Dexpanthenol is considered safe during breastfeeding, but consult a healthcare provider for specific recommendations.

Storage

Store at room temperature, away from light and moisture. Keep out of reach of children.

Formulations

• Topical cream
• Topical ointment
• Topical solution

Indications

• Dermatitis
• Acne
• Rosacea
• Hyperpigmentation
• Skin aging

Dosage

Children: Refer to the BNF for Children for specific dosing guidelines for paediatric patients.

Adults: Refer to the BNF for specific dosing guidelines based on the condition being treated.

Mechanism of action

Niacinamide functions primarily as a precursor to NAD and NADP, which are crucial for numerous enzymatic reactions in the body. It is involved in the NAD salvage pathway, which recycles nicotinamide for NAD synthesis. This process is vital for cellular energy production and metabolic processes. Niacinamide also has anti-inflammatory properties, which may contribute to its effects in skin health.

Pharmacodynamics

Niacinamide exhibits various pharmacological effects, including enhancing skin barrier function, reducing inflammation, and improving skin pigmentation. It has been shown to modulate keratinocyte function, improve collagen synthesis, and decrease the synthesis of sebum, thereby providing beneficial effects in conditions like acne and rosacea.

Pharmacokinetics

Niacinamide is readily absorbed from the gastrointestinal tract. It is distributed widely throughout the body and can cross biological membranes. The metabolism of niacinamide primarily occurs in the liver through methylation and conjugation, and it is excreted in urine as metabolites. The half-life of niacinamide is approximately 1-2 hours, and its effects can be prolonged due to its role in NAD synthesis.

Pregnancy

No evidence of harm, but use only if clearly needed.

Breast-feeding

Considered safe to use while breastfeeding.

Storage

Store in a cool, dry place away from light.

Formulations

• {'type': 'Topical cream', 'concentration': 'Various concentrations available'}
• {'type': 'Oral tablets', 'concentration': '100 mg, 250 mg, 500 mg'}

Mechanism of action

Cyproheptadine appears to exert its antihistamine and antiserotonin effects by competing with free histamine and serotonin for binding at their respective receptors. Antagonism of serotonin on the appetite center of the hypothalamus may account for cyproheptadine's ability to stimulate the appetite. CYPROHEPTADINE...IS A SEROTONIN & HISTAMINE ANTAGONIST... ... It is an effective H1 blocker. Cyproheptadine also has prominent 5-H blocking activity on smooth muscle by virtue of its binding to 5-HT2A receptors. ... It has weak anticholinergic activity and possess mild central depressant properties.

Pharmacodynamics

Cyproheptadine has been observed to antagonize several pharmacodynamic effects of serotonin in laboratory animals, including bronchoconstriction and vasodepression, and has demonstrated similar efficacy in antagonizing histamine-mediated effects. The reason for its efficacy in preventing anaphylactic shock has not been elucidated, but appears to be related to its anti-serotonergic effects.

Mechanism of action

Dexpanthenol is an alcohol derivative of pantothenic acid, a component of the B complex vitamins and an essential component of a normally functioning epithelium. Dexpanthenol is enzymatically cleaved to form pantothenic acid, which is an essential component of Coenzyme A, which acts as a cofactor in many enzymatic reactions that are important for protein metabolism in the epithelium. Dermatological effects of the topical use of dexpanthenol include increased fibroblast proliferation and accelerated re-epithelialization in wound healing. Furthermore, it acts as a topical protectant, moisturizer, and has demonstrated anti-inflammatory properties. This alcohol ... is said to increase the amount of coenzyme A available for the synthesis of acetylcholine. Increased formation of acetylcholine is thought to increase peristalsis and intestinal tone. ... To test the functional effect of pantothenate on dermal fibroblasts, cells were cultured and in vitro proliferation tests were performed using a standardized scratch test procedure. For all three donors analyzed, a strong stimulatory effect of pantothenate at a concentration of 20 ug/mL on the proliferation of cultivated dermal fibroblasts was observed. To study the molecular mechanisms resulting in the proliferative effect of pantothenate, gene expression was analyzed in dermal fibroblasts cultivated with 20 ug/mL of pantothenate compared with untreated cells using the GeneChip Human Exon 1.0 ST Array. A number of significantly regulated genes were identified including genes coding for interleukin (IL)-6, IL-8, Id1, HMOX-1, HspB7, CYP1B1 and MARCH-II. Regulation of these genes was subsequently verified by quantitative real-time polymerase chain reaction analysis. Induction of HMOX-1 expression by pantothenol and pantothenic acid in dermal cells was confirmed on the protein level using immunoblots. Functional studies revealed the enhanced suppression of free radical formation in skin fibroblasts cultured with panthenol. In conclusion, these studies provided new insight in the molecular mechanisms linked to the stimulatory effect of pantothenate and panthenol on the proliferation of dermal fibroblasts. /Calcium pantotenate/ ... Pantothenic acid, pantothenol and other derivatives ... are precursors of CoA /that/ protect cells and whole organs against peroxidative damage by increasing the content of cell glutathione...

Pharmacodynamics

Pantothenic acid is a precursor of coenzyme A, which serves as a cofactor for a variety of enzyme-catalyzed reactions involving transfer of acetyl groups. The final step in the synthesis of acetylcholine consists of the choline acetylase transfer of acetyl group from acetylcoenzyme A to choline. Acetylcholine is the neurohumoral transmitter in the parasympathetic system and as such maintains the normal functions of the intestine. Decrease in acetylcholine content would result in decreased peristalsis and in extreme cases adynamic ileus.