Pharmacology Specifics – First Generation Antipsychotics Flashcards
What are the 11 FDA approved indications for the use of antipsychotics?
Schizophrenia bipolar disorder major depressive disorder (adjunctive therapy) Tourette's syndrome severe behavioral problems hyperactivity anxiety hiccups acute intermittent porphyria Nausea/vomiting Tetanus
What are the seven non-FDA approved uses for antipsychotics?
Dementia (behavioral disturbances)
substance use disorder (reduction in use)
anorexia nervosa (increase body weight) obsessive-compulsive disorder
posttraumatic stress disorder
generalized anxiety disorder
What is the mechanism of action for both first and second generation antipsychotics with regard to dopamine receptors?
They block post-synaptic D2 dopamine receptors in the mesolimbic system, which has been associated with their antipsychotic effect
What is another name for antipsychotics?
Neuroleptics
How do the first generation and second generation antipsychotics differ in their mechanism of action on serotonin receptors?
First generation antipsychotics minimally antagonize serotonin receptors; whereas the second-generation antipsychotics have greater antagonism of serotonin receptors
The side effects associated with first and second generation antipsychotics are due to antagonism at which three types of receptors?
Histaminic, muscarinic, and Alpha-adrenergic receptors
Which generation of antipsychotics are more frequently associated with significant adverse side effects, such as extrapyramidal symptoms (EPS)? What is this due to?
First generation antipsychotics
This is due to their higher antagonism of D2 dopamine receptors
Thorazine
Chlorpromazine
Who makes all first generation antipsychotics?
Multiple generic manufacturers
Except Orap (pimozide) which is manufactured by Teva and brand-name only
What is the route and form of Thorazine? What is the recommended dosage per day?
PO, tablets
200-1000 mg per day
BID or TID
Prolixin
Fluphenazine
What is the route and form of Prolixin?
PO, IM
Tablets, liquid IM, acute IM, depot
What is the recommended PO, IM acute, and IM depot doses of Prolixin?
PO
0.5-20 mg per day,
Often given BID with doses larger than 10 mg
IM acute
5-10 mg Q6-8 hrs PRN
IM depot
12.5-25 mg Every 2 weeks
Haldol
Haloperidol
What route and forms does Haldol come in?
PO, IM
Tablets, liquid IM, acute IM, depot
What are the recommended PO, intramuscular acute, and intramuscular depot doses of Haldol?
PO: 0.5-20 mg per day
Intramuscular, acute: 5-10 mg Q6-8 hrs PRN
Intramuscular, depot: 50-200 mg given once monthly
What’s the difference between the intramuscular depot shot for Prolixin, and that for Haldol?
The dose for Prolixin is 12.5-25 mg, while the dose for Haldol is 50-200 mg
Haldol is given once monthly, while Prolixin is given every two weeks
Loxitane
Loxapine
Navane
Thiothixene
Which two first generation antipsychotics can be dispensed in capsule form?
Navane and Loxitane
What is the route of administration for Loxitane? What is the recommended daily dose?
PO
25-250 mg per day
What is the route of administration for Navane? What is the recommended daily dose?
PO
15-30 mg per day
Which is more expensive, Loxitane or Navane?
Loxitane
Trilafon
Perphenazine
Orap
Pimozide
Mellaril
Thioridazine
Stelazine
Trifluoperazine
What route and form are Trilafon, Orap, Mellaril, and Stelazine dispensed in?
PO; tablets
What is the recommended daily dose for Trilafon?
16-64 mg per day
What is the recommended daily dose for Orap?
1-10 mg per day
What is the recommended daily dose for Stelazine?
2-40 mg per day
What is the recommended daily dose for Navane?
15-30 mg per day
What is the recommended daily dose for Mellaril?
200-800 mg per day
Which first generation antipsychotic in tablet form is the cheapest?
Haldol
Which first generation antipsychotics in the tablet form is the second cheapest?
Prolixin
Which 2 first generation antipsychotic in the tablet form is the most expensive?
Orap and Trilafon
How should first generation antipsychotics be adjusted in patients with renal insufficiency or renal failure?
No dosage adjustment needed
With regard to pregnancy, what category are the first generation antipsychotics in?
Category C
How should the dosage of first generation antipsychotics be adjusted for patients with liver failure or liver disease?
They should be used with caution in patients with liver disease, especially chlorpromazine and perphenazine because they are both metabolized by the liver
What are the two options for the starting recommended dose of Thorazine?
10 mg
3-4 times per day
25 mg
2-3 times per day
How should Thorazine be increased?
One can increase by 20-50 mg per day
What is the maximum recommended dose of Thorazine per day?
400 mg
What is the recommended intramuscular dose of Thorazine?
Intramuscular dose is 25 mg
It can be repeated in 1 hour if needed
What’s the recommended starting oral dose of Haldol? How much should it be increased per day?
1 mg per day or twice daily
It should be increased by 1-2 mg per day
What’s the maximum recommended dose of Haldol per day?
100 mg per day
What’s the initial, recommended long-acting intramuscular dose of Haldol?
10-20 times the total oral dose
What should be done if the initial long-acting intramuscular dose of Haldol is greater than 100mg?
It should be administered in separate doses one week apart
After giving the initial dose, the following month, what dose of long-acting intramuscular Haldol should be given?
10-15 times the total oral dose
What’s the maximum, recommended, long-acting intramuscular dose of Haldol?
450 mg
What is the recommended starting dose of Orap? How should the dose be gradually increased?
The recommended initial dose is 1-2 mg per day in divided doses
The dose should be gradually increased every other day
What is the maximum recommended dose per day of Orap?
10 mg
What type of biogenetic testing should be done for doses greater than 4 mg with the use of Orap?
CYP2D6 genotyping should be done
What is the recommended starting oral dose for Navane? What is the maximum recommended dose per day?
1-2 mg per day in divided doses
The maximum dose is 60 mg per day
What is the intramuscular dose of Navane?
4 mg, 2-3 times per day
Maximum dose of 60 mg per day
What is the recommended starting oral dose of Stelazine? What is the maximum dose per day?
2-5 mg twice per day
The maximum dose is 40 mg per day divided doses
What is the recommended intramuscular dose of Stelazine? What is the maximum dose given per day?
An intramuscular dose of 1-2 mg can be given every 4-6 hours as needed
The maximum dose is 6 mg per day
What is the recommended starting dose of Prolixin? What is the maximum dose per day?
2.5-10 mg per day in divided doses every 6-8 hours
The maximum dose is 40 mg per day
What is the conversion from oral dosing to intramuscular dosing for Prolixin?
The intramuscular dose is 1.25 times the oral dose every 2-4 weeks