Table 1.
Commercially available drugs for the treatment of AD.
| Drugs | Trade Name (Company) | Action Mechanism | Dosage Form |
Dose | LogP (Permeability) Molecular Weight (M.W) (g/mol) | K (Partition Coefficient) |
|---|---|---|---|---|---|---|
| Tacrine | Cognex (Sciele, Atlanta, GA, USA) | Reversible inhibition of acetylcholinesterase (AChE) | Capsule | Initial dose: 10 mg orally q.i.d (between meals if possible) for 6 weeks. Maintenance dose: may increase to 20 mg orally q.i.d. Further increases to 120 mg and 160 mg/day may be done in 6-week intervals. |
2.71 M.W = 234.72 |
|
| Donepezil | Aricept (Pfizer, New York City, NY, USA) | Reversible inhibitor of acetylcholinesterase which prevents the hydrolysis of acetylcholine. | Tablet | 5 mg q.d., may increase to 10 mg/day after 4–6 weeks if tolerated, then to 23 mg/day after at least 3 months | 4.7 M.W = 379.5 |
log Kow = 4.86 (est) |
| Rivastigmine | Exelon (Novartis, Basel, Switzerland) |
Inhibits the hydrolytic activity of AChE and BChE and binds to catalytic sites. | Solution Capsule |
Oral Solution and capsules 6 mg to 12 mg per day, administered b.i.d. (daily doses of 3 mg to 6 mg b.i.d.) | 2.3 M.W = 250.34 |
|
| Galantamine | Razadyne (Janssen, Beerse, Belgium) | Binds reversibly to acetylcholine esterase and enhances the intrinsic action of acetylcholine on nicotinic receptors. | Tablet Capsule Oral solution |
Tablets contain 4 mg, 8 mg, and 12 mg galantamine. Capsules contain 8 mg, 16 mg, and 24 mg galantamine. Oral solution contains 4 mg galantamine (as 5.13 mg galantamine hydrobromide) per mL. |
1.8 M.W = 287.35 |
|
| Memantine | Namenda (Allergan, Dublin, Ireland) | N-methyl D-aspartate (NMDA) antagonist | Tablet Oral solution |
Tablets: 5 mg q.d., may increase to 10 mg/day, 15 mg/day, and 20 mg/day at 1-week intervals if tolerated Oral solution: same as above |
3.28 M.W = 179.3 |
log Kow = 3.28 |
| Memantine and Donepezil | Namzaric (Actavis, Parsippany, NJ, USA) | N-methyl D-aspartate (NMDA) antagonist plus cholinesterase inhibitor | Capsule (ER) | 7 mg memantine/10 mg donepezil q.d., may increase to 28 mg memantine/10 mg donepezil in 7 mg increments at 1-week intervals if tolerated | M.W = 215.76 | |
| Aducanumab | Aduhelm (Biogen, Cambridge, MA, USA) | Targets accumulated Aβ plaques | Intravenous infusion | Doses 1 and 2 (weeks 0 and 4)—1 mg/kg IV over one hour Doses 3 and 4 (weeks 8 and 16—3 mg/kg IV over one hour |
M.W = 145,912.34 |