1 Spring 2022_PL Psychotropics for Alzheimer’s disease Neurotransmitters Acetylcholine (ACH) – neurotransmitter of the parasympathetic nervous system, which controls muscles, memory, and coordination; changes in acetylcholine levels are involved with Alzheimer’s disease (too little acetylcholine) Glutamate– an excitatory neurotransmitter; relay of sensory information; allows controlled amount of calcium into nerve cells Psychotropic medications for treating patient with Alzheimer’s disease exert their effects in various ways by influencing synaptic transmission: Enzyme inhibitors Drugs that inhibit catabolic enzymes promote excess buildup of the neurotransmitter in the synapse. Receptor blockade (antagonists) Some drugs cause receptor blockade, thereby resulting in a reduction in transmission and decreased neurotransmitter activity. These drugs are called antagonists. Neurotransmitter Acetylcholine (ACH) Note: Catabolized by the enzyme acetylcholinesterase Glutamate Function memory, movement, sleep, arousal Relay of sensory information Excitatory Neurotransmitter Possible Link ↓ levels : Alzheimer’s disease Psychotropic Medications Acetylcholinesterase inhibitors – Inhibit the enzyme that breaks down ACH Examples No direct link May prolong life of neurons NMDA receptor antagonists act by blocking NMDA receptors from Memantine (Namenda) Donepezil (Aricept) 2 Spring 2022_PL Acetylcholinesterase inhibitors Indications • Acetylcholinesterase inhibitors may be used to treat Alzheimer disease to improve cognitive function in the early stages. Actions • Some of the symptoms of AD are thought to be the result of a deficiency of the neurotransmitter acetylcholine (ACH). In the brain, acetylcholine is inactivated by the enzyme acetylcholinesterase. • Acetylcholinesterase inhibitors slow down the degradation of acetylcholine, thereby increasing concentrations of the neurotransmitter in the brain. o o o Donepezil (Aricept) Galantamine (Razadyne) Rivastigmine (Exelon) The client with Alzheimer’s disease has decreased acetylcholine. The enzyme, acetylcholinesterase is inhibited from destroying acetylcholine. Nursing Considerations Most common side effects are diarrhea, dizziness, fatigue, and headache. • Donepezil (Aricept): May slow the heart rate by means of its cholinergic effect. • Galantamine (Razadyne): Can also cause bronchoconstriction and is used with caution in clients with asthma and COPD. • Rivastigmine (Exelon): Used with caution in clients with peptic ulcer disease, bradycardia, sick sinus syndrome, urinary obstruction, and lung disease, because it enhances cholinergic transmission, thereby intensifying symptoms of these disorders. NMDA receptor antagonist NMDA receptor antagonist is used to slow down the progression of cognitive decline and function. It is used in the later stage of Alzheimer’s disease. NMDA receptor antagonists act by blocking NMDA receptors from excessive glutamate, preventing continuous influx of calcium into nerve cells, and ultimately slowing down neuronal degradation. Slows down brain cell death. o Memantine (Namenda) Glutamate is an excitatory neurotransmitter and speeds neuron activity. By blocking receptors from glutamate, the life of neurons may be prolonged. 3 Spring 2022_PL