Andogablin Actions

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Actions of Andogablin in details

The action of the drug on the human body is called Pharmacodynamics in Medical terminology. To produce its effect and to change the pathological process that is happening the body and to reduce the symptom or cure the disease, the medicine has to function in a specific way. The changes it does to the body at cellular level gives the desired result of treating a disease. Drugs act by stimulating or inhibiting a receptor or an enzyme or a protein most of the times. Medications are produced in such a way that the ingredients target the specific site and bring about chemical changes in the body that can stop or reverse the chemical reaction which is causing the disease.
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Pharmacology: Andogablin is a γ-aminobutyric acid analogue.

Mechanism of Action: Andogablin binds with high affinity to the α2-δ site (an auxiliary subunit of voltage-gated calcium channels) in central nervous system tissues. Although the mechanism of action of Andogablin is unknown, results with genetically modified mice and with compounds structurally related to Andogablin suggest that binding to the α -δ subunit may be involved in Andogablin's antinociceptive and antiseizure effects in animal models.

While Andogablin is a structural derivative of the inhibitory neurotransmitter γ-aminobutyric acid (GABA), it does not bind directly to GABAA, GABAB, or benzodiazepine receptors, does not augment GABAA responses in cultured neurons, does not alter rat brain GABA concentration or have acute effects on GABA uptake or degradation.

Pharmacokinetics: Andogablin is well-absorbed after oral administration, is eliminated largely by renal excretion and has an elimination half-life (t½) of about 6 hrs. Following oral administration of Andogablin capsules under fasting conditions, peak plasma concentrations occur within 1.5 hrs. Andogablin oral bioavailability is >90% and is independent of dose. Following single (25-300 mg) and multiple dose (75-900 mg/day) administration, maximum plasma concentrations (Cmax) and area under the plasma concentration-time curve (AUC) values increase linearly. Following repeated administration, steady-state is achieved within 24-48 hrs. Multiple-dose pharmacokinetics can be predicted from single-dose data.

The rate of Andogablin absorption is decreased when given with food, resulting in a decrease in Cmax of approximately 25-30% and an increase in time to reach maximum plasma concentration (Tmax) to approximately 3 hrs. However, administration of maxpregabalin with food has no clinically relevant effect on the total absorption of Andogablin. Therefore, Andogablin can be taken with or without food. Andogablin does not bind to plasma proteins. The apparent volume of distribution of Andogablin following oral administration is approximately 0.5 L/kg.

Andogablin undergoes negligible metabolism in humans. Following a dose of radiolabeled Andogablin, approximately 90% of the administered dose was recovered in the urine as unchanged Andogablin. The N-methylated derivative of Andogablin, the major metabolite of Andogablin found in urine, accounted for 0.9% of the dose.

Andogablin is eliminated from the systemic circulation primarily by renal excretion as unchanged drug with a mean elimination t½ of 6.3 hrs in subjects with normal renal function. Mean renal clearance was estimated to be 67-80.9 mL/min in young healthy subjects. Because Andogablin is not bound to plasma proteins this clearance rate indicates that renal tubular reabsorption is involved. Andogablin elimination is nearly proportional to creatinine clearance (CrCl). No specific pharmacokinetic studies were carried out in patients with impaired liver function. Since Andogablin does not undergo significant metabolism and is excreted predominantly as unchanged drug in the urine, impaired liver function would not be expected to significantly alter Andogablin plasma concentrations.

Andogablin oral clearance tended to decrease with increasing age. This decrease in Andogablin oral clearance is consistent with age-related decreases in CrCl. Pharmacokinetics of Andogablin have not been adequately studied in pediatric patients.

How should I take Andogablin?

Take Andogablin exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.

You may take Andogablin with or without food.

Measure liquid medicine with a special dose-measuring spoon or medicine cup, not with a regular table spoon. If you do not have a dose-measuring device, ask your pharmacist for one.

Do not change your dose of Andogablin without your doctor's advice. Tell your doctor if the medication does not seem to work as well in treating your condition.

Call your doctor if you have any problems with your vision while taking Andogablin. If you are taking Andogablin to prevent seizures, keep taking it even if you feel fine. You may have an increase in seizures if you stop taking Andogablin. Follow your doctor's instructions. Do not stop using Andogablin without first talking to your doctor, even if you feel fine. You may have increased seizures or withdrawal symptoms such as headache, sleep problems, nausea, and diarrhea. Ask your doctor how to avoid withdrawal symptoms when you stop using Andogablin. Wear a medical alert tag or carry an ID card stating that you take Andogablin. Any medical care provider who treats you should know that you take seizure medication.

Store at room temperature away from moisture, light, and heat.

Andogablin administration

Administration of drug is important to know because the drug absorption and action varies depending on the route and time of administration of the drug. A medicine is prescribed before meals or after meals or along with meals. The specific timing of the drug intake about food is to increase its absorption and thus its efficacy. Few work well when taken in empty stomach and few medications need to be taken 1 or 2 hrs after the meal. A drug can be in the form of a tablet, a capsule which is the oral route of administration and the same can be in IV form which is used in specific cases. Other forms of drug administration can be a suppository in anal route or an inhalation route.
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Take exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.

You may take Andogablin with or without food.

Measure liquid medicine with a special dose-measuring spoon or medicine cup, not with a regular table spoon. If you do not have a dose-measuring device, ask your pharmacist for one.

Do not change your dose of Andogablin without your doctor's advice. Tell your doctor if the medication does not seem to work as well in treating your condition.

Call your doctor if you have any problems with your vision while taking Andogablin.

If you are taking Andogablin to prevent seizures, keep taking it even if you feel fine. You may have an increase in seizures if you stop taking Andogablin. Follow your doctor's instructions.

Do not stop using Andogablin without first talking to your doctor, even if you feel fine. You may have increased seizures or withdrawal symptoms such as headache, sleep problems, nausea, and diarrhea. Ask your doctor how to avoid withdrawal symptoms when you stop using Andogablin.

Wear a medical alert tag or carry an ID card stating that you take Andogablin. Any medical care provider who treats you should know that you take seizure medication.

Store at room temperature away from moisture, light, and heat.

Andogablin pharmacology

Pharmacokinetics of a drug can be defined as what body does to the drug after it is taken. The therapeutic result of the medicine depends upon the Pharmacokinetics of the drug. It deals with the time taken for the drug to be absorbed, metabolized, the process and chemical reactions involved in metabolism and about the excretion of the drug. All these factors are essential to deciding on the efficacy of the drug. Based on these pharmacokinetic principles, the ingredients, the Pharmaceutical company decides dose and route of administration. The concentration of the drug at the site of action which is proportional to therapeutic result inside the body depends on various pharmacokinetic reactions that occur in the body.
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Mechanism of Action

Andogablin (Andogablin) binds with high affinity to the alpha2-delta site (an auxiliary subunit of voltage-gated calcium channels) in central nervous system tissues. Although the mechanism of action of Andogablin has not been fully elucidated, results with genetically modified mice and with compounds structurally related to Andogablin (such as gabapentin) suggest that binding to the alpha2-delta subunit may be involved in Andogablin's anti-nociceptive and antiseizure effects in animals. In animal models of nerve damage, Andogablin has been shown to reduce calcium-dependent release of pro-nociceptive neurotransmitters in the spinal cord, possibly by disrupting alpha2-delta containing-calcium channel trafficking and/or reducing calcium currents. Evidence from other animal models of nerve damage and persistent pain suggest the anti-nociceptive activities of Andogablin may also be mediated through interactions with descending noradrenergic and serotonergic pathways originating from the brainstem that modulate pain transmission in the spinal cord.

While Andogablin is a structural derivative of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), it does not bind directly to GABAA, GABAB, or benzodiazepine receptors, does not augment GABAA responses in cultured neurons, does not alter rat brain GABA concentration or have acute effects on GABA uptake or degradation. However, in cultured neurons prolonged application of Andogablin increases the density of GABA transporter protein and increases the rate of functional GABA transport. Andogablin does not block sodium channels, is not active at opiate receptors, and does not alter cyclooxygenase enzyme activity. It is inactive at serotonin and dopamine receptors and does not inhibit dopamine, serotonin, or noradrenaline reuptake.

Pharmacokinetics

Andogablin is well absorbed after oral administration, is eliminated largely by renal excretion, and has an elimination half-life of about 6 hours.

Absorption and Distribution

Following oral administration of Andogablin capsules under fasting conditions, peak plasma concentrations occur within 1.5 hours. Andogablin oral bioavailability is ≥90% and is independent of dose. Following single- (25 to 300 mg) and multiple- dose (75 to 900 mg/day) administration, maximum plasma concentrations (Cmax) and area under the plasma concentration-time curve (AUC) values increase linearly. Following repeated administration, steady state is achieved within 24 to 48 hours. Multiple-dose pharmacokinetics can be predicted from single-dose data.

The rate of Andogablin absorption is decreased when given with food, resulting in a decrease in Cmax of approximately 25% to 30% and an increase in Tmax to approximately 3 hours. However, administration of Andogablin with food has no clinically relevant effect on the total absorption of Andogablin. Therefore, Andogablin can be taken with or without food.

Andogablin does not bind to plasma proteins. The apparent volume of distribution of Andogablin following oral administration is approximately 0.5 L/kg. Andogablin is a substrate for system L transporter which is responsible for the transport of large amino acids across the blood brain barrier. Although there are no data in humans, Andogablin has been shown to cross the blood brain barrier in mice, rats, and monkeys. In addition, Andogablin has been shown to cross the placenta in rats and is present in the milk of lactating rats.

Metabolism and Elimination

Andogablin undergoes negligible metabolism in humans. Following a dose of radiolabeled Andogablin, approximately 90% of the administered dose was recovered in the urine as unchanged Andogablin. The N-methylated derivative of Andogablin, the major metabolite of Andogablin found in urine, accounted for 0.9% of the dose. In preclinical studies, Andogablin (S-enantiomer) did not undergo racemization to the R-enantiomer in mice, rats, rabbits, or monkeys.

Andogablin is eliminated from the systemic circulation primarily by renal excretion as unchanged drug with a mean elimination half-life of 6.3 hours in subjects with normal renal function. Mean renal clearance was estimated to be 67.0 to 80.9 mL/min in young healthy subjects. Because Andogablin is not bound to plasma proteins this clearance rate indicates that renal tubular reabsorption is involved. Andogablin elimination is nearly proportional to creatinine clearance (CLcr).

Pharmacokinetics in Special Populations

Race

In population pharmacokinetic analyses of the clinical studies in various populations, the pharmacokinetics of Andogablin were not significantly affected by race (Caucasians, Blacks, and Hispanics).

Gender

Population pharmacokinetic analyses of the clinical studies showed that the relationship between daily dose and Andogablin drug exposure is similar between genders.

Renal Impairment and Hemodialysis

Andogablin clearance is nearly proportional to creatinine clearance (CLcr). Dosage reduction in patients with renal dysfunction is necessary. Andogablin is effectively removed from plasma by hemodialysis. Following a 4-hour hemodialysis treatment, plasma Andogablin concentrations are reduced by approximately 50%. For patients on hemodialysis, dosing must be modified.

Elderly

Andogablin oral clearance tended to decrease with increasing age. This decrease in Andogablin oral clearance is consistent with age-related decreases in CLcr. Reduction of Andogablin dose may be required in patients who have age-related compromised renal function.

Pediatric Pharmacokinetics

Pharmacokinetics of Andogablin have not been adequately studied in pediatric patients.

Drug Interactions

In Vitro Studies

Andogablin, at concentrations that were, in general, 10-times those attained in clinical trials, does not inhibit human CYP1A2, CYP2A6, CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A4 enzyme systems. In vitro drug interaction studies demonstrate that Andogablin does not induce CYP1A2 or CYP3A4 activity. Therefore, an increase in the metabolism of coadministered CYP1A2 substrates (e.g. theophylline, caffeine) or CYP 3A4 substrates (e.g., midazolam, testosterone) is not anticipated.

In Vivo Studies

The drug interaction studies described in this section were conducted in healthy adults, and across various patient populations.

Gabapentin

The pharmacokinetic interactions of Andogablin and gabapentin were investigated in 12 healthy subjects following concomitant single-dose administration of 100-mg Andogablin and 300-mg gabapentin and in 18 healthy subjects following concomitant multiple-dose administration of 200-mg Andogablin every 8 hours and 400-mg gabapentin every 8 hours. Gabapentin pharmacokinetics following single- and multiple-dose administration were unaltered by Andogablin coadministration. The extent of Andogablin absorption was unaffected by gabapentin coadministration, although there was a small reduction in rate of absorption.

Oral Contraceptive

Andogablin coadministration (200 mg three times a day) had no effect on the steady-state pharmacokinetics of norethindrone and ethinyl estradiol (1 mg/35 µg, respectively) in healthy subjects.

Lorazepam

Multiple-dose administration of Andogablin (300 mg twice a day) in healthy subjects had no effect on the rate and extent of lorazepam single-dose pharmacokinetics and single-dose administration of lorazepam (1 mg) had no effect on the steady-state pharmacokinetics of Andogablin.

Oxycodone

Multiple-dose administration of Andogablin (300 mg twice a day) in healthy subjects had no effect on the rate and extent of oxycodone single-dose pharmacokinetics. Single-dose administration of oxycodone (10 mg) had no effect on the steady-state pharmacokinetics of Andogablin.

Ethanol

Multiple-dose administration of Andogablin (300 mg twice a day) in healthy subjects had no effect on the rate and extent of ethanol single-dose pharmacokinetics and single-dose administration of ethanol (0.7 g/kg) had no effect on the steady-state pharmacokinetics of Andogablin.

Phenytoin, carbamazepine, valproic acid, and lamotrigine

Steady-state trough plasma concentrations of phenytoin, carbamazepine and carbamazepine 10,11 epoxide, valproic acid, and lamotrigine were not affected by concomitant Andogablin (200 mg three times a day) administration.

Population pharmacokinetic analyses in patients treated with Andogablin and various concomitant medications suggest the following:

Therapeutic class Specific concomitant drug studied
Concomitant drug has no effect on the pharmacokinetics of Andogablin
Hypoglycemics Glyburide, insulin, metformin
Diuretics Furosemide
Antiepileptic Drugs Tiagabine
Concomitant drug has no effect on the pharmacokinetics of Andogablin and Andogablin has no effect on the pharmacokinetics of concomitant drug
Antiepileptic Drugs Carbamazepine, lamotrigine, phenobarbital, phenytoin, topiramate, valproic acid



References

  1. DailyMed. "PREGABALIN: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
  2. NCIt. "Pregabalin: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).
  3. EPA DSStox. "Pregabalin: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).

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