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US Approved OTC

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Investigational

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Primary Target

Adenosine A1 receptor

4

Adenosine A2a receptor

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Adenosine A2b receptor

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Phosphodiesterase 1

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Beta amyloid A4 protein

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Highest Phase

Approved

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Phase II

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Approval Year

1921

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Unknown

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Condition

Apnea of prematurity

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Atopic dermatitis

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Drowsiness

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Migraine

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Alzheimer’s disease

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Treatment Modality

Primary

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Palliative

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CNS Active

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CNS Penetrant

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Originator

Staedeler, G.|Frerichs, F.T.

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Chemical

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EPA CompTox

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NCI_THESAURUS

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ATC Level 1

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DIAGNOSTIC AGENTS

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PSYCHOANALEPTICS

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ATC Level 3

OTHER DIAGNOSTIC AGENTS

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PSYCHOSTIMULANTS, AGENTS USED FOR ADHD AND NOOTROPICS

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ATC Level 4

Tests for gastric secretion

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Xanthine derivatives

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Salts, Hydrates, Esters, etc.

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CAFFEINE

3G6A5W338E

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Status:

US Approved OTC

First marketed in 1921

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Adenosine A2a receptor

Adenosine A2b receptor

Phosphodiesterase 1

Adenosine A1 receptor

Conditions:

Atopic dermatitis

Apnea of prematurity

Caffeine is a methylxanthine alkaloid found in the seeds, nuts, or leaves of a number of plants native to South America and East Asia that is structurally related to adenosine and acts primarily as an adenosine receptor antagonist with psychotropic a...

nd anti-inflammatory activities. Upon ingestion, caffeine binds to adenosine receptors in the central nervous system (CNS), which inhibits adenosine binding. This inhibits the adenosine-mediated downregulation of CNS activity; thus, stimulating the activity of the medullary, vagal, vasomotor, and respiratory centers in the brain. The anti-inflammatory effects of caffeine are due the nonselective competitive inhibition of phosphodiesterases. Caffeine is used by mouth or rectally in combination with painkillers (such as aspirin and acetaminophen) and a chemical called ergotamine for treating migraineheadaches. It is also used with painkillers for simple headaches and preventing and treating headaches after epidural anesthesia. Caffeine creams are applied to the skin to reduce redness and itching in dermatitis. Healthcare providers sometimes give caffeine intravenously (by IV) for headache after epidural anesthesia, breathing problems in newborns, and to increase urine flow. In foods, caffeine is used as an ingredient in soft drinks, energy drinks, and other beverages.

SCYLLO-INOSITOL

1VS4X81277

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Status:

Investigational

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Beta amyloid A4 protein

Conditions:

Alzheimer’s disease

Scyllo-inositol (ELND005) is an inositol isoform. Inositol is a derivative of cyclohexane with six hydroxyl groups, making it a polyol. It also is known as a sugar alcohol, having exactly the same molecular formula as glucose or other hexoses. Scyllo...

-inositol (ELND005) is a naturally occurring plant sugar alcohol found most abundantly in the coconut palm. It appears to accumulate in a number of human tissues and biofluids through dietary consumption. It has traditionally been considered to be a B vitamin although it has an uncertain status as a vitamin and a deficiency syndrome has not been identified in man. Although scyllo-inositol (ELND005) at pharmacologic doses may alter myo-inositol levels and indirectly affect phosphatidyl-inositol signaling, its main effects are thought to be binding and inhibition of beta-amyloid 42 peptide aggregation and formation of beta-amyloid fibrils. In transgenic animals, scyllo-inositol (ELND005) reduced brain beta-amyloid concentrations and plaque burden, preserved synaptic density, and improved learning deficits. Scyllo-inositol (ELND005) also appears to neutralize toxic effects of beta-amyloid oligomers, including amelioration of oligomer-induced synaptic loss, long-term potentiation inhibition, and memory deficits. Scyllo-inositol (ELND005) is an attractive candidate as a potential disease-modifying oral treatment for Alzheimer disease.

caffeine sodium iodide

7DU9VK8U6A

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Status:

US Approved OTC

First marketed in 1921

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Adenosine A2a receptor

Adenosine A2b receptor

Phosphodiesterase 1

Adenosine A1 receptor

Conditions:

Atopic dermatitis

Apnea of prematurity

Caffeine is a methylxanthine alkaloid found in the seeds, nuts, or leaves of a number of plants native to South America and East Asia that is structurally related to adenosine and acts primarily as an adenosine receptor antagonist with psychotropic a...

nd anti-inflammatory activities. Upon ingestion, caffeine binds to adenosine receptors in the central nervous system (CNS), which inhibits adenosine binding. This inhibits the adenosine-mediated downregulation of CNS activity; thus, stimulating the activity of the medullary, vagal, vasomotor, and respiratory centers in the brain. The anti-inflammatory effects of caffeine are due the nonselective competitive inhibition of phosphodiesterases. Caffeine is used by mouth or rectally in combination with painkillers (such as aspirin and acetaminophen) and a chemical called ergotamine for treating migraineheadaches. It is also used with painkillers for simple headaches and preventing and treating headaches after epidural anesthesia. Caffeine creams are applied to the skin to reduce redness and itching in dermatitis. Healthcare providers sometimes give caffeine intravenously (by IV) for headache after epidural anesthesia, breathing problems in newborns, and to increase urine flow. In foods, caffeine is used as an ingredient in soft drinks, energy drinks, and other beverages.

CAFFEINE MONOHYDRATE

9T65I06326

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Status:

US Approved OTC

First marketed in 1921

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Adenosine A2a receptor

Adenosine A2b receptor

Phosphodiesterase 1

Adenosine A1 receptor

Conditions:

Atopic dermatitis

Apnea of prematurity

Caffeine is a methylxanthine alkaloid found in the seeds, nuts, or leaves of a number of plants native to South America and East Asia that is structurally related to adenosine and acts primarily as an adenosine receptor antagonist with psychotropic a...

nd anti-inflammatory activities. Upon ingestion, caffeine binds to adenosine receptors in the central nervous system (CNS), which inhibits adenosine binding. This inhibits the adenosine-mediated downregulation of CNS activity; thus, stimulating the activity of the medullary, vagal, vasomotor, and respiratory centers in the brain. The anti-inflammatory effects of caffeine are due the nonselective competitive inhibition of phosphodiesterases. Caffeine is used by mouth or rectally in combination with painkillers (such as aspirin and acetaminophen) and a chemical called ergotamine for treating migraineheadaches. It is also used with painkillers for simple headaches and preventing and treating headaches after epidural anesthesia. Caffeine creams are applied to the skin to reduce redness and itching in dermatitis. Healthcare providers sometimes give caffeine intravenously (by IV) for headache after epidural anesthesia, breathing problems in newborns, and to increase urine flow. In foods, caffeine is used as an ingredient in soft drinks, energy drinks, and other beverages.

CAFFEINE CITRATE

U26EO4675Q

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Status:

US Approved OTC

First marketed in 1921

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Adenosine A2a receptor

Adenosine A2b receptor

Phosphodiesterase 1

Adenosine A1 receptor

Conditions:

Atopic dermatitis

Apnea of prematurity

Caffeine is a methylxanthine alkaloid found in the seeds, nuts, or leaves of a number of plants native to South America and East Asia that is structurally related to adenosine and acts primarily as an adenosine receptor antagonist with psychotropic a...

nd anti-inflammatory activities. Upon ingestion, caffeine binds to adenosine receptors in the central nervous system (CNS), which inhibits adenosine binding. This inhibits the adenosine-mediated downregulation of CNS activity; thus, stimulating the activity of the medullary, vagal, vasomotor, and respiratory centers in the brain. The anti-inflammatory effects of caffeine are due the nonselective competitive inhibition of phosphodiesterases. Caffeine is used by mouth or rectally in combination with painkillers (such as aspirin and acetaminophen) and a chemical called ergotamine for treating migraineheadaches. It is also used with painkillers for simple headaches and preventing and treating headaches after epidural anesthesia. Caffeine creams are applied to the skin to reduce redness and itching in dermatitis. Healthcare providers sometimes give caffeine intravenously (by IV) for headache after epidural anesthesia, breathing problems in newborns, and to increase urine flow. In foods, caffeine is used as an ingredient in soft drinks, energy drinks, and other beverages.

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