Equivalence and Substitution

Regulations fall within the jurisdiction of the individual states.

Pharmaceutical equivalence: same active ingredient, same dosage form, same route of administration, identical in dosage strength or concentration, may contain different excipients 

Therapeutic equivalence:  pharmaceutical equivalence and bioequivalent 

Bioequivalence | ADME

A = absorption

D = distribution

M = metabolism

E = elimination 

The manufacturer must submit graphs to the FDA illustrating the two products containing the same drug have similar blood concentration vs. time curves, including: 

Time to peak

Peak concentrations

Area under the curve (AUC)

References

Approved Drug Products with Therapeutic Equivalence Evaluations aka The Orange Book

The Electronic Orange Book (internet version)

United States Pharmacopeia Dispensing Information (USP/DI) Volume III plus supplements 

Facts and Comparisons, Inc Approved Bioequivalence Codes 

FDA’s Internet Website http://www.fda.gov

Drugs marketed before 1938 are not required to be in The Orange Book.

A Rated

Bioequivalent to the innovator’s drug product 

Therapeutically equivalent to the brand name or reference product

A-rated products may be substituted for one another.

B Rated

NOT bioequivalent to the innovator’s drug product 

B-rated products may not be substituted for one another.

Generally, a tablet cannot be substituted for a capsule, an ointment for a cream.  Most sustained-release or controlled-release are not interchangeable. 

AB Rated

Previously not considered to be bioequivalent and now organized into bioequivalence groups (AB1, AB2, AB3, etc)

Must have the same number or lack of number to be bioequivalent 

Cannot substitute an AB1 product for a product designated as AB2

The Federal government has not passed regulations limiting the substitution of these products although a few states have.

Examples:

Carbamazepine

Digoxin

Levothyroxine

Lithium

Phenytoin

Theophylline

Valproic acid

Warfarin

Checkout our self-guided courses and instant download study guides on Teachable for Texas, Iowa, Maryland and federal law!

Drug Approval Process

My tests had several questions that referenced to the drug approval process. I suggest that anyone planning to take the MPJE for any state be familiar with the drug approval processes

Investigational New Drug Application

•1stapplication before drug is given to humans

•Federal Drug Administration (FDA) has 30 days to decide if suitable for testing

•Must provide clinical protocols to be used in human testing

Clinical Trials

Initiated after FDA approves the investigational new drug application

3 phases before marketing and 1 phase after marketing

Phase 1: Small group of healthy individuals to evaluate toxicity, kinetics, safety

Phase 2: Large group (100+) with the disease being treated to evaluate effectiveness, safety, and adverse drug events (ADEs)

Phase 3: Large group (1000+) to evaluate effectiveness, double-blinded with placebo

Phase 4: Post-marketing surveillance to determine if drug should stay on the market

New Drug Application (NDA)

Can apply once data on safety, efficacy, toxicity, stability, production methods, packaging and clinical trial data exists

Typically takes 6 months for review 

Abbreviated New Drug Application (ANDA)

For introducing a generic of an already approved drug

Requires proof of kinetics, bioequivalence/bioavailability

Supplemental New Drug Application (SNDA)

For changes to synthesis, production, manufacturer location, packaging and/or labeling

For new dose form, strength or therapeutic use

Epidiolex – What is it? Is it a controlled substance?

What is it?

First and only FDA-approved prescription cannabidiol (CBD)

What is it used for?

Seizures associated with Lennox-Gastaut syndrome (LGS), Dravet syndrome or tuberous sclerosis complex (TSC)

Mechanism of action for the reduction of seizures is unknown.

How is it dosed and taken?

Titrated dosing given orally or via feeding tube (non PVC) twice daily, administered consistently with or without food.

LGS or Dravet syndrome:

Initial dose: 5mg/kg/day (2.5mg/kg twice daily)

Recommended dosing: 10 to 15mg/kg/day (5 to 7.5mg/kg twice daily) increased in weekly increments of 5mg/kg/day (2.5mg/kg twice daily)

Maximum dosing: 20mg/kg/day (10mg/kg twice daily) 

TSC:

Initial dose: 5mg/kg/day (2.5mg/kg twice daily)

Recommended dosing: 10 to 20mg/kg/day (5 to 10mg/kg twice daily) increased in weekly increments of 5mg/kg/day (2.5mg/kg twice daily)

Maximum dosing: 25mg/kg/day (12.5mg/kg twice daily) 

If rapid titration is necessary, dose may be increased no more frequently than every other day.
Dose adjustment and a slower titration is recommended in patients with moderate to severe hepatic impairment.
Should not be stopped suddenly due to the risk of increased frequency of seizures and status epilepticus. 

Recommended lab work: 

Transaminase and bilirubin levels prior to starting treatment, at month 1, month 3 and month 6 then periodically thereafter.

Patients on valproate or are at increased risk of elevated transaminase levels and/or hepatocellular injury.  

If levels are elevated, consider a dose reduction or discontinuation of Epidiolex or other medications known to increase transaminase levels such as valproate and/or clobazam.  

Common side effects (> 10% and greater than placebo): transaminase elevations, somnolence, fatigue, malaise, asthenia, decreased appetite, diarrhea, vomiting, pyrexia, rash, insomnia and infections.

Other important side effects to be aware of: suicidal behavior and ideation

Potential interactions to consider:

Several potential drug-drug interactions to consider, most commonly run into potential drug-drug interactions with other anticonvulsant medications:

Clobazam, diazepam, & valproate

Recommended to counsel patient or caregiver on signs/symptoms to watch for and recommend lab work as appropriate.  

Strawberry flavored but does not contain strawberry.

Compatible with a ketogenic diet.

Federal law no longer considers Epidiolex to be a controlled substance.  It had originally been federally scheduled as a CV.  Now it is federally non-controlled.  There are a handful of states that have it scheduled as a controlled substance.  

https://www.drugtopics.com/view/dea-deschedules-antiepileptic-cbd-oral-solution-epidiolex

Controlled StatusState
CIVLouisiana
CVFlorida
CVGeorgia
CVIdaho
CVMaryland
CVMontana
CVNebraska
CVNorth Dakota
CVPuerto Rico
Controlled Substance Status of Epidiolex (all other states are non-controlled)