Drug monograph

Attached is an example of the assignment. My drug is Finerenone (Kerendia)

Almotriptan
I. Description
Almotriptan maleate is a selective serotonin (5-HT) 1B/1D receptor agonist. (1) It has a
high and specific affinity for these receptors. It acts selectively at human cranial vessels.
It has little activity at peripheral arteries. (2)
II. Indication
Axert (almotriptan maleate) was given FDA approval on May 7, 2001 (Application
number 021001) for the treatment of acute migraine. (3)
III. Dosage/Administration
Axert comes as either 6.25 or 12.5mg tablets. Starting doses need to be individualized.
In clinical trials 12.5mg was equivalent to 50mg sumatriptan. If after the first dose, the
headache returns, another dose may be taken after 2 hours. No more than 2 doses in 24
hours should be taken (maximum 25mg/d). Dose should be adjusted in hepatic or renal
impairment to a starting dose of 6.25mg and a maximum of 12.5mg/24h. (1)
IV. Pharmacology
Almotriptan binds with high affinity to serotonin (5-HT) 1B/1D receptors. Binding causes
vasoconstriction of the extracerebral intracranial blood vessels that theoretically become
vasodilated during an acute migraine. It has weak affinity for serotonin (5-HT) 1A and
serotonin (5-HT) 7 receptors. It has no significant affinity for serotonin (5-HT) 2,
serotonin (5-HT) 3, serotonin (5-HT) 4, or serotonin (5-HT) 6 receptors. (1) Table 1
shows the relative potency of the serotonin (5-HT) 1B/1D receptor agonists at cranial
versus coronary arteries.
Table 1: Relative Potencies of Serotonin (5-HT) 1B/1D Receptor Agonists (4)
Potency at Vascular serotonin (5-HT) Receptors (nM)
Drug
Cranial Arteries
Coronary Arteries
7.52
NA
Almotriptan
6.3-7.2
5.4
Eletriptan
7.86
7.38
Frovatriptan
6.8-7.15
6.77-6.9
Naratriptan
6.3-7.05
6.35
Rizatriptan
6.0-7.15
5.8-6.7
Sumatriptan
6.4-6.9
6.1-7.3
Zolmitriptan
NA=Not published
V. Pharmacokinetics
Almotriptan is well absorbed after oral administration with peak plasma levels 1-3 hours
after administration. It is minimally protein bound and eliminated primarily via secretion
in the urine (approximately 75%). It is metabolized to inactive metabolites by one minor
and two major pathways. Monoamine oxidase A (MAO-A) deamination, which is
approximately 27% of a dose, and cytochrome P450 (3A4, 2D6) (CYP 450) oxidation,
which is approximately 12% of a dose, are the major routes. Flavin monooxygenase is
the minor route. Forty percent of a dose is excreted unchanged in the urine. Table 2
compares the pharmacokinetic parameters for the serotonin (5-HT) 1B/1D receptor
agonists.
Table 2: Pharmacokinetics of Serotonin (5-HT) 1B/1D Receptor Agonists (4)
Drug
Cmax
ng/ml
tmax
h
F
%
t 1/2
h
Sumatriptan
54-78.4
14
Almotriptan
49.5
Eletriptan
107190
4.2-7.0
7.814.4
20
1.3-4.7
1.52.3
1.43.8
1.01.5
2-4
0.84.1
1-3
0.56.0
Frovatriptan
Naratriptan
Rizatriptan
Zolmitriptan
2
Protein
binding
%
14-21
Metabolic
Enzyme
Major/minor
MAO-A
70-80
3.0-3.7
35
50
3.6-6.9
24-30
63-74
40-45
40-49
Vd
L/kg
Liposolubility
2.4-3.3
Cl
ml/min/k
g
3.5-3.9
2.5
8.6
HIGH*
NR
CYP 3A4 MAOA/CYP 2D6
CYP 3A4
2.4
6.6
HIGH
25
4.5-6.6
NR
38-31
NR
CYP various
3-4
2.4-2.9
1.9-3.1
2.7-3.8
NR
HIGH
1.8-3
1.5-3.5
14
25
MAO-A
CYP 1A2 MAOA
1.3-2.5
7.0-8.3
3.2-5.3
2.0-3.1
HIGH
HIGH
LOW
* See Tfelt-Hansen (5)
VI.
Adverse Reactions
The most common adverse events possibly related to almotriptan in a 1 year open label
clinical trial were vomiting, somnolence, dizziness, fatigue, and nausea (