Anti-Androgens Flashcards
What drugs are in the Anti-Androgens class?
Drugs in this class are:
- Flutamide
- Abiraterone acetate
- Apalutamide
- Bicalutamide
- Enzalutamide
- Nilutamide
- Darolutamide
What is the brand name of Flutamide?
The brand name of this generic drug is:
- Eulexin
What is the brand name of Abiraterone acetate?
The brand name of this generic drug is:
- Yonsa
- Zytiga
What is the brand name of Apalutamide?
The brand name of this generic drug is:
- Erleada
What is the brand name of Bicalutamide?
The brand name of this generic drug is:
- Casodex
What is the brand name of Enzalutamide?
The brand name of this generic drug is:
- Xtandi
What is the brand name of Nilutamide?
The brand name of this generic drug is:
- Nilandron
What is the brand name of Darolutamide?
The brand name of this generic drug is:
- Nubeqa
What is the generic of name of Eulexin?
The generic name of this brand name drug is:
- Flutamide
What is the generic of name of Yonsa?
The generic name of this brand name drug is:
- Abiraterone acetate
What is the generic of name of Zytiga?
The generic name of this brand name drug is:
- Abiraterone acetate
What is the generic of name of Erleada?
The generic name of this brand name drug is:
- Apalutamide
What is the generic of name of Casodex?
The generic name of this brand name drug is:
- Bicalutamide
What is the generic of name of Xtandi?
The generic name of this brand name drug is:
- Enzalutamide
What is the generic of name of Nilandron?
The generic name of this brand name drug is:
- Nilutamide
What is the generic of name of Nubeqa?
The generic name of this brand name drug is:
- Darolutamide
What are the main/common indications of the Anti-Androgens class?
The main/common indications of this drug class are:
- Prostate cancer
What is the class and MOA of Flutamide?
This drug in the following class:
- Anti-Androgens
This drug’s MOA is as follows:
- Non-steroidal anti-androgen that inhibits androgen uptake and inhibits binding of androgen in target tissues
What is the class and MOA of Abiraterone acetate?
This drug in the following class:
- Anti-Androgens
This drug’s MOA is as follows:
- Selectively and irreversibly inhibits CYP17 an enzyme required for biosynthesis and inhibits the formation of testosterone
What is the class and MOA of Apalutamide?
This drug in the following class:
- Anti-Androgens
This drug’s MOA is as follows:
- Nonsteroidal androgen receptor antagonist
What is the class and MOA of Bicalutamide?
This drug in the following class:
- Anti-Androgens
This drug’s MOA is as follows:
- Selectively and irreversibly inhibits CYP17 an enzyme required for biosynthesis and inhibits the formation of testosterone
What is the class and MOA of Enzalutamide?
This drug in the following class:
- Anti-Androgens
This drug’s MOA is as follows:
- Pure androgen receptor signaling inhibitor
What is the class and MOA of Nilutamide?
This drug in the following class:
- Anti-Androgens
This drug’s MOA is as follows:
- Non-steroidal anti-androgen that inhibits androgen uptake and inhibits binding of androgen in target tissues
What is the class and MOA of Darolutamide?
This drug in the following class:
- Anti-Androgens
This drug’s MOA is as follows:
- Competitive androgen receptor inhibitor, also inhibits androgen receptor translocation and androgen receptor-mediated transcription
What are the notable/common monitoring parameters for the Anti-Androgens class?
The notable/common monitoring parameters for this drug class are:
- Serum transaminases at baseline, monthly for 4 months. and periodically thereafter: monitor liver function tests at the first sign or symptom of liver dysfunction
- Prostate specific antigen (PSA) to monitor response to therapy
Describe the emetic potential of the Anti-Androgens class.
The emetic potential of this drug class is:
- N/A (minimal)
Describe the metabolism of the Anti-Androgen class.
The metabolism of this drug class is as follows:
- Extensively hepatic
What are the notable/common ADRs of the Anti-Androgens class?
The notable/common ADRs of this drug class are:
- Headache
- Peripheral edema
- Hot flashes
- Gynecomastia
- Secondary infections
What are the clinical pearls of Flutamide?
The clinical pearls of this drug are as follows:
- See common pearls for class
- Used in combination with a GNRH agonist
- Response rate = 50-87%
What are the clinical pearls of Abiraterone acetate?
The clinical pearls of this drug are as follows:
- See common pearls for class
- Approved for metastatic, castration-resistant prostate cancer in combination with a steroid BID.
- Co-administration with the recommended dose of steroid compensates for drug-induced reductions in serum cortisol and blocks the compensatory increase in adrenocorticotropic hormone seen with this drug
What are the clinical pearls of Bicalutamide?
The clinical pearls of this drug are as follows:
- See common pearls for class
- Used in combination with a GNRH agonist
- Response rate = 54-70%
What are the clinical pearls of Enzalutamide?
The clinical pearls of this drug are as follows:
- See common pearls for class
- Requires dose adjustments for strong CYP2C8 inhibitors and CYP3A4 inducers
What are the clinical pearls of Nilutamide?
The clinical pearls of this drug are as follows:
- See common pearls for class
- Used in combination with orchiectomy
- Response rate = 40%
What are the clinical pearls of the Anti-Androgens class?
The clinical pearls of this drug class are as follows:
- Monotherapy is less effective than GNRH agonist therapy and is not currently recommended to be used alone (unless patient had orchiectomy)
- Therefore, used in combination with androgen ablation therapy
- Overall efficacy is similar, but bicalutamide is generally preferred due to better toxicity profile
Describe the dosing schedule and administration for the anti-androgen class.
Dosing schedule and administration for drug class:
- All are given PO
- All are given once daily except:
- Flutamide (TID)
- Abiraterone acetate (BID)
- Darolutamide (BID)
Describe the dosing schedule and administration for flutamide.
Dosing schedule and administration for this drug:
- PO TID
Describe the dosing schedule and administration for abiraterone acetate.
Dosing schedule and administration for this drug:
- PO BID
Describe the dosing schedule and administration for apalutamide.
Dosing schedule and administration for this drug:
- PO once daily
Describe the dosing schedule and administration for bicalutamide.
Dosing schedule and administration for this drug:
- PO once daily
Describe the dosing schedule and administration for enzalutamide.
Dosing schedule and administration for this drug:
- PO once daily
Describe the dosing schedule and administration for nilutamide.
Dosing schedule and administration for this drug:
- PO once daily
Describe the dosing schedule and administration for darolutamide.
Dosing schedule and administration for this drug:
- PO BID