framycetin, phenylephrine, and gramicidin

Action and Spectrum

Actions and Spectrum: 

Mechanism of Action:  

framycetin belongs to the class of antibiotics known as aminoglycosides. It inhibits bacterial protein synthesis by binding to the bacterial ribosome, specifically the 30S subunit. This binding prevents the proper formation of the bacterial protein chain, inhibiting bacterial growth. 

phenylephrine is a selective alpha-1 adrenergic receptor agonist. It constricts the blood vessels in the nasal mucosa, leading to vasoconstriction and reduced nasal congestion. 

gramicidin is a peptide antibiotic that disrupts bacterial cell membranes. It forms channels within the bacterial membrane, leading to the leakage of ions and other molecules. This disruption of the bacterial membrane integrity ultimately results in cell death. 

Spectrum of Activity:  

framycetin has a broad-spectrum activity against many Gram-positive and Gram-negative bacteria. In intranasal use, it can help target bacterial pathogens that may be causing nasal infections. 

phenylephrine primarily acts locally to relieve nasal congestion. It does not have direct antibacterial activity. 

gramicidin primarily acts against Gram-positive bacteria. It is not effective against Gram-negative bacteria due to the presence of an outer membrane, which limits its access to the bacterial cell. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Increased blood pressure 

Tachycardia 

Dizziness 

Dry mucous membranes 

Cardiac arrhythmia 

Palpitations 

Depression 

Drowsiness 

Stinging sensation in the nose 

Black Box Warning

Black box warning: 

None 

Contraindication / Caution

Contraindications/caution: 

Contraindications: 

• Allergy or Hypersensitivity: The intranasal solution should not be used if an individual has a known allergy or hypersensitivity to any components. 
• Severe Cardiovascular Disease: phenylephrine, a component of the intranasal solution, can cause vasoconstriction and potentially increase blood pressure.  
• Closed-Angle Glaucoma: phenylephrine can cause pupillary dilation, precipitating an acute attack of closed-angle glaucoma in susceptible individuals. It is contraindicated in individuals with a history of closed-angle glaucoma. 
• Urinary retention: phenylephrine, due to its vasoconstrictive effects, may worsen urinary retention in individuals with conditions such as prostatic hypertrophy or bladder neck obstruction. 

Caution: 

• Systemic Effects: phenylephrine, when used intranasally, can have systemic effects such as increased heart rate, increased blood pressure, and potential cardiovascular effects.  
• Local Irritation: The intranasal solution may cause local irritation or discomfort, such as stinging, burning, or nasal dryness.  
• Drug Interactions: The components of the intranasal solution may have potential interactions with other medications. 

Pregnancy / Lactation

Pregnancy consideration: Insufficient data available 

Lactation: Excretion of the drug in human breast milk is unknown 

Pregnancy category: 

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

framycetin is an antibiotic that inhibits bacterial protein synthesis by binding to the bacterial ribosome. This inhibitory action leads to the suppression of bacterial growth and the elimination of susceptible bacteria. 

phenylephrine is a selective alpha-1 adrenergic receptor agonist. Stimulating alpha-1 adrenergic receptors on the blood vessels in the nasal mucosa causes vasoconstriction, reducing nasal congestion and swelling. 

gramicidin is a peptide antibiotic that disrupts bacterial cell membranes by forming channels or pores within the membrane. This disruption leads to the leakage of ions and molecules, ultimately resulting in bacterial cell death. 

Pharmacodynamics:  

Combining framycetin, phenylephrine, and gramicidin in an intranasal solution provides a multifaceted approach to address nasal infections, congestion, and inflammation. framycetin helps combat bacterial pathogens, phenylephrine is a decongestant by reducing nasal swelling and congestion, and gramicidin may have additional antibacterial activity against Gram-positive bacteria. 

Pharmacokinetics: 

Absorption 

When applied intranasally, framycetin may have limited systemic absorption. Its action primarily occurs at the application site, targeting bacterial pathogens in the nasal cavity. 

phenylephrine can be absorbed systemically when applied intranasally, although the extent of absorption is relatively low compared to oral administration. Its vasoconstrictive effects primarily occur locally in the nasal mucosa. gramicidin, when applied intranasally, may have minimal systemic absorption. Its primary action occurs at the site of application within the nasal cavity.  

Distribution 

framycetin remains primarily localized at the administration site, exerting its antibacterial effects in the nasal cavity. Once absorbed, phenylephrine is distributed throughout the body via the bloodstream. Still, it primarily acts locally within the nasal mucosa. gramicidin remains primarily localized at the administration site, exerting its antibacterial effects in the nasal cavity.  

Metabolism 

framycetin is minimally metabolized in the body. It is primarily excreted unchanged. phenylephrine undergoes extensive first-pass metabolism in the liver, forming inactive metabolites. gramicidin is a peptide and is not significantly metabolized in the body.  

Elimination and Excretion 

The elimination of framycetin occurs mainly via renal excretion, where it is excreted unchanged in the urine. Metabolized phenylephrine and its metabolites are primarily excreted through the kidneys. The excretion of gramicidin occurs primarily via renal excretion without significant biotransformation. 

Adminstartion

Administration: 

Intranasal administration 

• Shake the bottle well to ensure uniform mixing of the components. 
• Remove the cap from the bottle. 
• Insert the bottle’s nozzle into one nostril while closing the other nostril with a finger. 
• Squeeze the bottle to release the recommended number of drops or spray into the nostril. Follow the specific instructions regarding the dosage and number of drops/sprays. 
• Breathe gently through the nose while administering the drops/spray to ensure the solution reaches the desired area. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: framycetin, phenylephrine, and  gramicidin 

Why do we use framycetin, phenylephrine, and gramicidin? 

The combined formulation of framycetin, phenylephrine, and gramicidin in an intranasal solution may be used for various nasal congestion, inflammation, and infection indications.  

• Nasal Congestion: The intranasal solution can temporarily relieve nasal congestion caused by allergies, sinusitis, or the common cold. phenylephrine acts as a nasal decongestant by constricting blood vessels in the nasal passages, reducing swelling and congestion. 
• Rhinitis: The formulation may alleviate rhinitis symptoms, including nasal congestion, sneezing, and runny nose, especially in cases where bacterial infection is suspected. framycetin and gramicidin provide antibacterial activity to target potential bacterial pathogens contributing to the symptoms. 
• Nasal Infections: The combined solution may help treat nasal infections caused by susceptible bacteria. framycetin and gramicidin have broad-spectrum antibacterial activity against various Gram-positive and Gram-negative bacteria, helping to eliminate the infection. 
• Sinusitis: In sinusitis, which is inflammation or infection of the sinuses, the intranasal solution may provide relief by reducing nasal congestion, inflammation, and potential bacterial infection.