Guaranine - General Information
A methylxanthine naturally occurring in some beverages and also used as a pharmacological agent. Guaranine&
Pharmacology of Guaranine
Guaranine, a naturally occurring xanthine derivative like theobromine and the bronchodilator theophylline, is used as a CNS stimulant, mild diuretic, and respiratory stimulant (in neonates with apnea of prematurity). Often combined with analgesics or with ergot alkaloids, caffeine is used to treat migraine and other headache types. Over the counter, caffeine is available to treat drowsiness or mild water-weight gain.
Guaranine for patients
Parents/caregivers of patients receiving CAFCIT® (caffeine citrate) should receive the following instructions:
1. CAFCIT® does not contain any preservatives and each vial is for single use only. Any unused portion of the medication should be discarded.
2. It is important that the dose of CAFCIT® be measured accurately, i.e., with a 1 cc or other appropriate syringe.
3. Consult your physician if the baby continues to have apnea events; do not increase the dose of CAFCIT® without medical consultation.
4. Consult your physician if the baby begins to demonstrate signs of gastrointestinal intolerance, such as abdominal distention, vomiting, or bloody stools, or seems lethargic.
5. CAFCIT® should be inspected visually for particulate matter and discoloration prior to its administration. Vials containing discolored solution or visible particulate matter should be discarded.
(caffeine citrate) Oral Solution
Each bottle (vial) of CAFCIT contains a total of 60 mg of caffeine citrate in 3 mL (20 mg/mL).
Information and Instructions for Use
This leaflet tells you about CAFClT (KAF-sit) and how to give it to your baby. Read the following information before giving this medicine to your baby. Completely discuss CAFCIT with your baby's doctor. Continue to discuss any questions you have about this medicine at your baby's checkups.
After you remove your baby's dose, throw away the open bottle (vial) and all medicine left in it. Use each vial of CAFCIT for only one dose. There will be extra medicine left in the vial after one dose is removed. Leftover medicine should not be used because CAFCIT does not contain preservatives. Once the vial is open, any medicine that is not used right away must be discarded.
What is CAFCIT?
The main ingredient of CAFCIT is caffeine citrate. CAFCIT is a clear, colorless, medicine to treat apnea of prematurity - short periods when premature babies stop breathing. Apnea of prematurity is due to the baby's breathing centers not being fully developed.
How do I give CAFCIT to my baby?
Give CAFCIT to your baby once a day, at about the same time each day. Your baby's doctor will prescribe the right amount of CAFCIT based on your baby's weight and age. Carefully follow the doctor's dosing instructions.
Measure the dose of CAFCIT carefully. Your baby's doctor, nurse, or pharmacist will give you a suitable syringe or supply of syringes to measure small but accurate doses of CAFCIT.
Never change (increase or decrease) your baby's dose without speaking to your baby's doctor.
If your baby continues to have periods of apnea, call your baby's doctor right away.
CAFCIT can be swallowed by mouth or given through a feeding tube. Based on your baby's own situation, your baby's doctor or other healthcare professional should teach you how to give CAFCIT correctly.
CAFCIT should be clear and colorless. Before giving CAFCIT, look for small particles, cloudiness, or discoloration in the medicine. Do not use vials that contain cloudy or discolored medicine, or any visible particles.
CAFCIT does NOT contain any preservatives. Do not open the vial until it is time for your baby to receive the dose of medicine. Use each vial only once. After you remove your baby's dose, throw away the vial and all medicine left in the opened vial.
Ten (10) vials of CAFCIT are packaged in a child-resistant container. CAFClT vials are NOT CHILD-RESISTANT. Always store vials of CAFCIT in the child-resistant container. Follow the instructions below to open the child-resistant container, to open a vial of CAFCIT, and to remove a dose of medicine from the vial.
To open the child-resistant container that holds the vials of CAFCIT:
(Instructions with pictures are also printed on the top of the container)
- Hold the bottom-half of the child-resistant container with one hand and push the lower semicircular section on the front of the container with your thumb.
- With your other hand, pull the cover up until you hear it click.
- While holding the ends of the bottom-half of the container with both hands, place both index fingers on the two semicircular locking tabs on the sides of the container.
- Press the two tabs and raise the cover up.
To open a vial of CAFCIT (caffeine citrate):
- Hold the blue plastic top between the thumb and index finger. Use your thumb to flip the blue plastic top completely off the vial.
- Carefully lift up the metal ring.
- Pull the metal ring away from the vial and then pull it down towards the bottom of the vial without twisting the ring.
- After you pull the ring down and the metal band around the top of the vial is completely broken through, carefully remove the rest of the metal band by pulling it out and away from the vial.
- Being careful not to spill any medicine, remove the rubber stopper from the top of the vial.
To remove the prescribed dose from the vial:
You will need a small syringe to measure the exact amount of medicine that your baby's doctor prescribed. Your baby's doctor, nurse or pharmacist will give you this small syringe. Note that a milliliter (mL) is the same as a cubic centimeter (cc).
- Insert the tip of the syringe in the medicine and pull up on the plunger to draw the medicine into the syringe. Remove slightly more of the medicine than the exact amount to be given to your baby.
- Turn the syringe tip up so that any air in it rises to the top. Remove the air by gently pushing up on the syringe plunger. Continue to push the syringe plunger up to remove any extra medicine in the syringe, until only the exact number of milliliters (or cubic centimeters) that your baby's doctor prescribed remains in the syringe.
- Give the CAFCIT to your baby as your baby's doctor instructed.
- Throw away the sharp metal pieces, the rubber stopper, the open vial, and any medicine that remains in it after your baby receives the dose.
What are possible side effects of CAFCIT (caffeine citrate)?
Your baby may or may not develop side effects from taking CAFCIT. Each baby is different. If your baby develops one or more of the following symptoms, speak with your baby's doctor right away:
- restlessness, jitteriness or shakiness
- faster heart beat
- increased urination (increased diaper wetting)
The following symptoms may be caused by serious bowel or stomach problems. Call your baby's doctor right away if your baby develops:
- bloated abdomen (stomach area)
- bloody stools (bloody bowel movements)
- loss of energy, lethargy (acting sluggish)
This is not a complete list of side effects reported with CAFCIT. If you have a concern about your baby, speak with your baby's doctor. If you want more information about CAFCIT, speak with your baby's doctor or pharmacist.
Ben Venue Laboratories, Inc., Bedford, Ohio 44146.
Mead Johnson & Company, Evansville, IN 47721 U.S.A.
Mead JohnsonTM Nutritionals
©2003 Mead Johnson & Company Revised (2) May 2003
Cytochrome P450 1A2 (CYP1A2) is known to be the major enzyme involved in the metabolism of caffeine. Therefore, caffeine has the potential to interact with drugs that are substrates for CYP1A2, inhibit CYP1A2, or induce CYP1A2.
Few data exist on drug interactions with caffeine in preterm neonates. Based on adult data, lower doses of caffeine may be needed following coadministration of drugs which are reported to decrease caffeine elimination (e.g., cimetidine and ketoconazole) and higher caffeine doses may be needed following coadministration of drugs that increase caffeine elimination (e.g., phenobarbital and phenytoin).
Caffeine administered concurrently with ketoprofen reduced the urine volume in 4 healthy volunteers. The clinical significance of this interaction in preterm neonates is not known.
Interconversion between caffeine and theophylline has been reported in preterm neonates. The concurrent use of these drugs is not recommended.
CAFCIT® (caffeine citrate) is contraindicated in patients who have demonstrated hypersensitivity to any of its components.
Additional information about Guaranine
Guaranine Indication: For management of fatigue, orthostatic hypotension, and for the short term treatment of apnea of prematurity in infants.
Mechanism Of Action: Guaranine stimulates medullary, vagal, vasomotor, and respiratory centers, promoting bradycardia, vasoconstriction, and increased respiratory rate. This action was previously believed to be due primarily to increased intracellular cyclic 3′,5′-adenosine monophosphate (cyclic AMP) following inhibition of phosphodiesterase, the enzyme that degrades cyclic AMP. It is now thought that xanthines such as caffeine act as agonists at adenosine-receptors within the plasma membrane of virtually every cell. As adenosine acts as an autocoid, inhibiting the release of neurotransmitters from presynaptic sites but augmenting the actions of norepinephrine or angiotensin, antagonism of adenosine receptors promotes neurotransmitter release. This explains the stimulatory effects of caffeine. Blockade of the adenosine A1 receptor in the heart leads to the accelerated, pronounced "pounding" of the heart upon caffeine intake.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Caffeine
Synonyms: Caffeine, Anhydrous; Caffeine, Monohydrate; Caffeine, Synthetic; CFF; Cafeina; Caffein; Caffeine Pure; Compound 65; Methyltheobromide; Methyltheobromine; Monomethyl Derivative of Theophylline; Theobromine ME; Theophylline ME
Drug Category: Central Nervous System Stimulants; Anorexigenic Agents; Phosphodiesterase Inhibitors
Drug Type: Small Molecule; Approved
Other Brand Names containing Caffeine: Alert-Pep; Anoquan; Cafamil; Cafcit; Cafecon; Cafergot; Caffedrine; Caffedrine Caplets; Caffine; Cafipel; Coffein; Coffeine; Darvon Compound; Darvon Compound-65; Dasin; Dexitac; Dexitac Stay Alert Stimulant; Dhc Plus; Diurex; Durvitan; Eldiatric C; Enerjets; Ercatab; Esgic; Esgic-Plus; Femcet; Fioricet; Fiorinal; Guaranine; Hycomine; Invagesic; Invagesic Forte; Keep Alert; Kofein; Koffein; Lanorinal; Mateina; Maximum Strength Snapback Stimulant Powders; Medigesic Plus; Migergot; Miudol; Natural Caffeinum; Nix Nap; No-Doz; Nodaca; Nodoz Maximum Strength Caplets; Norgesic; Norgesic Forte; Organex; Orphengesic; Orphengesic Forte; Pep-Back; Phensal; Propoxyphene Compound 65; Propoxyphene Compound-65; Quick Pep; Refresh'n; SK 65 Compound; Stim; Synalgos-Dc; Thein; Theine; Triad; Ultra Pep-Back; Vivarin; Wake-Up; Wigraine;
Absorption: Readily absorbed after oral or parenteral administration. The peak plasma level for caffeine range from 6-10mg/L and the mean time to reach peak concentration ranged from 30 minutes to 2 hours.
Toxicity (Overdose): LD50=127 mg/kg (orally in mice)
Protein Binding: Low (25 to 36%).
Biotransformation: Hepatic cytochrome P450 1A2 (CYP 1A2) is involved in caffeine biotransformation. About 80% of a dose of caffeine is metabolized to paraxanthine (1,7-dimethylxanthine), 10% to theobromine (3,7-dimethylxanthine), and 4% to theophylline (1,3-dimethylxanthine).
Half Life: 3 to 7 hours in adults, 65 to 130 hours in neonates
Dosage Forms of Guaranine: Pill Oral
Solution / drops Oral
Tablet, extended release Oral
Chemical IUPAC Name: 1,3,7-trimethylpurine-2,6-dione
Chemical Formula: C8H10N4O2
Caffeine on Wikipedia: https://en.wikipedia.org/wiki/Caffeine
Organisms Affected: Humans and other mammals