A Game-Changer for Diabetes: Polymer Delivers Insulin Painlessly Through Skin
November 25, 2025
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Brand Name :
Numbrino, Goprelto
Synonyms :
cocaine
Class :
Local Anesthetics, Esters
Brand Name :
Numbrino, Goprelto
Synonyms :
cocaine
Class :
Local Anesthetics, Esters
Dosage Forms & Strengths 
Topical solution
4% (40mg/mL)
10% (100mg/mL)
Intranasal solution
4%
The dose varies between 40 and 160 mg, depending on the technique and the area of the nasal mucosa that needs to be anaesthetized
Each nasal cavity may receive up to 2 soaked cotton or rayon pledgets for a maximum dose of 160 mg)
Never use more than 3 mg/kg for a single procedure or surgery
Note:
When performing diagnostic procedures and surgeries on or via the nasal cavities in adults, it is recommended to provide this medication to induce local anaesthetic of the mucosal membranes
Recommended as a local (topical) anaesthetic for the oral, nasal, and laryngeal cavities exposed mucous membranes:
Use the lowest dose required to generate sufficient anaesthesia when using a 1–10% solution
Never go beyond 3 mg/kg or 300 mg
Dosage Forms & Strengths 
Topical solution
4% (40mg/mL)
Refer to adult dosing
may have an increased hypertensive effect when combined with sympathomimetics
may have an increased hypertensive effect when combined with sympathomimetics
CNS stimulants: they may increase the CNS depressant effect of antihistamines
CNS stimulants: they may increase the CNS depressant effect of antihistamines
CNS stimulants: they may increase the CNS depressant effect of antihistamines
CNS stimulants: they may increase the CNS depressant effect of antihistamines
dexchlorpheniramine, dextromethorphan, and phenylephrine
CNS stimulants: they may increase the CNS depressant effect of antihistamines
cocaine: they may increase the CNS depressant effect of CNS Depressants
cocaine: they may increase the CNS depressant effect of CNS Depressants
cocaine: they may increase the CNS depressant effect of CNS Depressants
cocaine: they may increase the CNS depressant effect of CNS Depressants
cocaine: they may increase the CNS depressant effect of CNS Depressants
may increase the hypertension effect of sympathomimetic drugs
may increase the hypertension effect of sympathomimetic drugs
may increase the hypertensive effects of sympathomimetics
acrivastine and pseudoephedrineÂ
may increase the hypertensive effects of sympathomimetics
may increase the hypertensive effect of sympathomimetics
may increase the antihypertensive effect of sympathomimetics
may increase the hypertensive effect of sympathomimetics
may increase the hypertensive effect of Sympathomimetics
may increase the hypertensive effect when combined
chlormethiazole: they may increase the CNS depressant effect of CNS stimulants
dexmedetomidine: they may increase the CNS depressant effect of CNS stimulants
lemborexant: they may increase the CNS stimulant effect of CNS stimulants
suvorexant: they may increase the CNS depressant effect of CNS Depressants
zolpidem: they may increase the CNS depressant effect of CNS Depressants
may increase the risk or severity of methemoglobinemia when miltefosine is combined
olopatadine: they may increase the CNS stimulant effect of CNS stimulants
flunarizine: they may increase the CNS depressant effect of CNS Depressants
kratom: they may increase the CNS depressant effect of CNS Depressants
it increases the toxicity of Norepinephrine Reuptake Inhibitors
it increases the toxicity of Norepinephrine Reuptake Inhibitors
it increases the toxicity of Norepinephrine Reuptake Inhibitors
it increases the toxicity of Norepinephrine Reuptake Inhibitors
it increases the toxicity of Norepinephrine Reuptake Inhibitors
may enhance the adverse/toxic effect of tricyclic antidepressants
it increases the toxicity of Norepinephrine Reuptake Inhibitors
it increases the toxicity of Norepinephrine Reuptake Inhibitors
it increases the toxicity of Norepinephrine Reuptake Inhibitors
it increases the toxicity of Norepinephrine Reuptake Inhibitors
it increases the toxicity of Norepinephrine Reuptake Inhibitors
The potential for methemoglobinemia to occur or its seriousness may be enhanced when mepartricin is used together with cocaine
When cyclacillin is used together with cocaine, this leads to increased risk or seriousness of methemoglobinemia
When ponesimod is used together with cocaine, this leads to enhanced risk or seriousness of bradycardia
When cocaine is used together with adenosine, this leads to enhanced risk or seriousness of QTc prolongation
when aclarubicin is combined with cocaine, there is an increased risk of methemoglobinemia
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the toxicity of Norepinephrine Reuptake Inhibitors
it increases the toxicity of Norepinephrine Reuptake Inhibitors
it increases the toxicity of Norepinephrine Reuptake Inhibitors
it increases the toxicity of Norepinephrine Reuptake Inhibitors
it increases the toxicity of Norepinephrine Reuptake Inhibitors
it increases the toxicity of Norepinephrine Reuptake Inhibitors
the risk of QTc prolongation may be increased
the neuromuscular blocking activity of cocaine may be increased
the risk of methemoglobinemia may be increased
the risk of methemoglobinemia may be increased
the risk of methemoglobinemia may be increased
the risk of methemoglobinemia may be increased
it increases the effect of hypertension of sympathomimetics
it increases the effect of hypertension of sympathomimetics
it increases the effect of hypertension of sympathomimetics
it increases the effect of hypertension of sympathomimetics
it increases the effect of hypertension of sympathomimetics
sorafenib increases the efficacy of cocaine by altering the hepatic CYP2B6 enzyme metabolism
Actions and Spectrum:
cocaine is a stimulant drug that is typically used recreationally for its euphoric effects. It is typically administered via inhalation, injection, or oral ingestion. Topical use of cocaine is not a common method of administration, and there is limited information available about its effects or safety when used in this way.
The drug can cause a range of effects including increased energy, increased alertness, and decreased appetite. However, it can also cause negative side effects such as increased blood pressure, heart rate, and body temperature. Additionally, long-term use of cocaine can lead to addiction and other serious health problems.
Frequency Defined 
1-10% 
Headache (3%)
Sinus tachycardia (2%)
Bradycardia (3%)
QT prolonged (3%)
Tachycardia (5%)
Epistaxis (1%)
QRS prolonged (2%)
>10% 
Hypertension (78%)
Contraindication/Caution:
Some potential contraindications or cautions for the use of cocaine topical include:
Pregnancy warnings:   
US FDA pregnancy category: C
Lactation:  
Excreted into human milk is unknown
Pregnancy Categories:        
Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester.
Category B: There were lack of studies on pregnant women and no evidence of risk to the foetus in animal experiments.
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 available 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: 
cocaine is a stimulant drug that is commonly used recreationally, but it also has some medical uses. Topical cocaine is a formulation of the drug that is applied to the skin. It is sometimes used as a local anesthetic for certain types of surgery, such as nasal or throat procedures. When applied topically, cocaine acts to numb the area where it is applied by blocking the transmission of nerve impulses. This can help to reduce pain and discomfort during medical procedures.
Pharmacodynamics: 
It works by increasing the levels of certain neurotransmitters, such as dopamine, in the brain. When used topically, cocaine is usually applied as a local anesthetic. When applied to the skin or mucous membranes, it causes a loss of sensation in the area by blocking the passage of nerve impulses. This is how it is used for medical procedures like nasal surgery. Topical cocaine also may cause vasoconstriction, which can help to reduce bleeding during surgery.
Pharmacokinetics:  
Absorption 
If applied topically, the absorption of cocaine would likely be low due to the drug’s low solubility in water and the barrier function of the skin.
Distribution 
However, if it can be absorbed, it will be distributed throughout the body via the bloodstream.
Metabolism
cocaine is rapidly metabolized in the liver and blood, primarily by the enzyme carboxylesterase.
Elimination and excretion 
The metabolites of cocaine are then excreted primarily in the urine
Administration: 
cocaine is a powerful stimulant drug that is typically administered through nasal inhalation, also known as snorting. It can also be administered through injection or smoking, but these methods are less common.
The effects of cocaine are immediate and can last for several hours. However, the drug has a high potential for addiction and can have serious side effects, including heart attack, stroke, and death. It is illegal to use or possess cocaine in most countries.
Patient information leaflet
Generic Name: cocaine
Why do we use cocaine?
cocaine is used for its stimulant effects, which can include increased energy, alertness, and euphoria. Some people use it to stay awake or to increase their ability to focus and perform tasks. Others use it recreationally for its euphoric effects and to feel a sense of euphoria and well-being.
However, it is important to note that cocaine is a highly addictive drug, and its use can have serious negative consequences on an individual’s physical and mental health, including addiction, heart attack, stroke, and death. Additionally, it is illegal to use or possess cocaine in most countries.
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