CENTRAL NERVOUS

SYSTEM DRUGS
 Nervous systems' major division

• Peripheral Nervous System (PNS)- monitors and coordinates

internal organ function and responds to changes in the
external environment.

• Central Nervous System (CNS)- responsible for sending,

receiving, processing and interpreting sensory information
and send information form all areas of the body. It also
receives information from and sends information to the
Peripheral Nervous System (PNS)
 BRAIN
The brain consists of 3 structurally distinct components:
First, the forebrain- It is also responsible for functions such as
receiving and processing sensory information, thinking, perceiving,
producing and understanding language, and controlling motor
function
Midbrain and hindbrain make up the brain stem and is
involved in auditory and visual responses as well as motor
function.
The midbrain also contains medulla oblongata while the hindbrain
extends from the spinal cord and composes of pons and
cerebellum
• Spinal cord- is a cylindrical bundle of nerves that is connected
to the brain, running down the protective spinal column,
extending from neck to the lower back.
• Neurons- are the basic units of nervous system. All cells of the
nervous system contains neurons, which in turn contain nerve
processes (“fingerlike” projections) that consist of axons and
dendrites.
 NERVOUS SYSTEM

CENTRAL NERVOUS SYSTEM PERIPHERAL NERVOUS

(INTEGRATIVE FUNCTIONS) SYSTEM

SOMATIC NERVOUS SYSTEM AUTONOMIC NERVOUS SYSTEM

(SKELETEAL MUSCLE (SMOOTH & CARDIAC MUSCLE AND
EFFECTORS) GLAND EFFECTORS)

SYMPATHETIC PARASYMPATHETIC
(FIGHT OR FLIGHT) (REST AND DIGEST)
Classes of Medications for treating CNS disorders

1. Analgesics
a. Opiods/Narcotics
b. NSAIDS (nonstreroidal anti-inflammatory drugs) and
paracetamol
2. Antiseizure/antiepileptic agents
3. Medications for neurodegenerative agents
4. Muscle relaxants
5. Local anesthetics
ANALGESICS
Analgesics and Pain Management
Analgesics is a broad term used to describe medications that provide
pain relief.
Primary classes: Narcotics
Non-narcotics (P-aminophenol der., NSAIDS)
I. NON-NARCOTICS
A. P-aminophenol derivative
1. Phenacetin- prodrug----> APAP (Acetaminophen)
-withdrawn due to nephrotoxicity and methemoglobinemia
2. Acetaminophen/Paracetamol- uses: Analgesic & Antipyretic; safe in
pregnant, lactating woman & among children.
T/E: Hepatotoxicity (hepatic necrosis), Nausea & vomiting, abdominal pain,
and jaundice
 B. NSAIDS- weak organic acids except Nabumetone
MOA: block COX ---> ↓PG synthesis
1. COX1- For PGs responsible for maintenance functions
2. COX2- Inducible enzymes; PGs for pain & inflammation
Classifications:
I. Non-selective
a. Aspirin- uses: Analgesic, Anti-inflammatory property,
Antipyretic, antiplatelet/antiaggregant
T/E: GI effects, Hypersensitivity reactions, effects in serum uric
acid level, CNS effects, Reye's syndrome
b. Indole derivative
ex: Indomethacin- inhibits COX1 & COX2; inhibits GI effects
use: mngt of Ductus Arteriosus
mngt of Barter's Syndrome
tx of pain in acute gout

c. Phenyl acetic derivatives

ex: True phenyl acetates- Sulindac, Diclofenac, Aceclofenac
Acetic Acid der.- Ketorolac, Etodolac, Nabumetone
d. Fenamates
ex: Mefenamic acid, Meclofenamic acid, Flofenamic acid
-Analgesics only; for acute pain only (NMT 5 days); never be
given to children

e. Propionic Acid Derivative

ex: Ibuprofen, Naproxen, Ketoprofen
-Analgesics & Anti-inflammatory
II. Selective & Specific COX-2 inhibitors
ex: Meloxicam- selective
-coxib - specific
T/E: ↑ risk of acute thrombotic events (stroke, MI)

II. NARCOTICS
Narcosis- stupor and insensibility
MOA: stimulate the release or mimic the action of endogenous
opiod peptides (enkephalins, dymorphins, endorphins,
endomorphins
Receptors: Mu, kappa, delta
Uses: Analgesics- Mild: Tramadol
Moderate: Codeine
Severe: Morphine
Management of Acute Pulmonary Edema

T/E: Tolerance (↑dose= same effect) -during 2-3weeks of chronic use

Addiction→ Physical dependence (withdrawal sx)
Convulsion
Respiratory depression
Classifications:
I. Based on sources
a. Natural (opiates)
i. Morphine- standard comparison as analgesic agent
-poor oral bioavailability (25-30%)
-40mg (po) = 10mg (IV)
ii. Codeine- standard comparison as anti-tussive agent
-weaker analgesic effect than morphine
iii. Thebaine- precursor in the synthesis of Naloxone
 b. Semi-synthetic (Opiods)
i. Heroin- aka diacetylmorphine/diamorphine
-common drug of abuse
ii. Semisynthetic morphine derivatives
e.g Hydromorphone,Oxymorphone
-8-12x more potent than codeine

c. Synthetic (Opiods)
i. Methadone- same efficacy with morphine
-good oral BA
-long DOA (less rapid of dev't of tolerance)
use: to wean-off of addicted to Morphine and Heroin
ii. Meperidine/Pethidine (Demerol)
-no cardiac & biliary effects
-used for acute pain only (NMT 5 days)
iii. Levorphanol
-5-7x more potent than morphine
iv. Tramadol
- weak der. of codeine
v. Fentanyl & related drugs (alfentanyl, sulfentanyl)
- 100x more potent than morphine
 Based on Pharmacodynamics:

a. Strong full agonists- morphine & its derivatives

b. Mild to Moderate Full Agonists- codeine & its derivatives

c. Partial Agonists- Nalbuphine, Butorphanol, Buprenorphine,

Pentazocine

d.Full Antagonists- Naloxone, Naltrexone, Nalmefene

ANTIPSYCHOTICS
& NEUROLEPTICS
 Schizoprenia- ↑ Dopamine ↑5HT
(+) (-)

Hallucination Alogia

Delusions Anhedonia

Disorganized speech Asociality

Bizarre behavior Flutting/Blunt effect

1.Typical/1st Generation
MOA: inhibits D2 receptor >>>> 5HT
-EPS- Extrapyrimidal symptom
e.g Phenothiazine, Butyrophenone, Thioxanthene

2. Atypical/2nd Generation
MOA: blocks 5HT >>> D2
e.g Clozapine, Olanzapine, Quetiapine,
ANTIDEPRESSANTS
Signs & Symptoms:
• anhedonia
• difficulty sleeping/ oversleeping
• lack of appetite
• worthlessness
• suicidal ideation
• asociality

1. Tricyclic Antidepressants (TCA)

use: MDD Major Depressive Disorder
SE: Excessive sedation, anticholinergic effects, weight gain
examples: Amitryptiline, Clomipramine, Imipramine
2. Selective Serotonin Reuptake Inhibitor (SSRI)
use: MDD, OCD, GAD, eating disorders, alcohol dependence
SE: ↑ suicidality
examples: Fluoxetine, Paroxetine, Escitalopram, Sertraline

3. Serotonin NE Reuptake Inhibitor (SNRI)

use: MDD, neurophatic pain
SE: hypertension (Venlafaxine), Hepatotoxic (Duloxetine)

4. Monoamine oxidase inhibitors

MAOa: metabolizes NE, Epi, 5HT, amines
MAOb: metabolizes Dopamine
Recall: MPITS
ANTICONVULSANTS/
SEDATIVES
Seizure: abnormal electrical activity in the brain
-simple vs complex
Types:
1. Simple partial seizure: conscious, jerking of body parts
2. Complex partial: jerking of body parts, loss of consciousness
3. Generalized Tonic Clonic seizure: (Grandmal)
Tonic phase: rigidity, LOC
Clonic phase: jerking of muscles, tongue biting, incontinence
4. Absence seizure (petitmal): “blank stares”, lip smacking
5. Myoclonic seizure
6. Status epilepticus
1. Phenytoin
uses: GTC, partial seizure, status epilepticus
SE: nystagmus, fetal hydantoin syndrome, hirsutism, diplopia

2. Carbamazepine
uses: GTC & partial seizure, bipolar disorder, trigeminal neuralgia
SE: Diplopia, SJS, Hyponatremia

3. Valproic acid
uses: DOC for BPD, GTC, absence (complicated)
SE: daytime sedation, weight gain, alopecia, teratogenic
4. Phenobarbital
uses: GTC, status epi, partial seizure, primary anti seizure for
children, infants, and pregnant women

5. Ethosuximide
use: simple absence
SE: behavioral changes

6. Benzodiazepines (Diazepam, Lorazepam, Clonazepam)

uses: status epilepticus, myoclonic seizure
7. Gabapentin
uses: Neuropathic pain, migraine

8. Lamotrigine
uses: DOC for partial seizure, BPD, myoclonic seizure

9. Levetiracetam
uses: GTC, partial

10. Topiramate
uses: migraine, GTC, partial seizure
Drugs for Parkinsons Disease
Parkinsons- neurodegenerative disease caused by
degeneration of dopaminergic neurons

1. Levodopa-carbidopa
use: 1st line for parkinsons dse
SE: GI upset, Behavioral changes

2. MAOb inhibitors (Selegiline, Rasagiline)

use: adjunct for PD
SE: Hypotension, insomnia
ANESTHETICS
I. GENERAL ANESTHETICS
-state characterized by unconsciousness, analgesia, amnesia,
loss of muscle reflexes

STAGES OF ANESTHESIA
1. Analgesia- decrease awareness to pain
2. Disinhibition- delirious, muscle excitation, amnesia, irregular
respiration, incontinence, vomiting
3. Surgical anesthesia- unconscious, no pain reflexes, no
muscle reflexes and contraction, stable vs
4. Medullary depression- severe CV and respiratory dep
ROUTES OF ADMINISTRATION
1. INHALATIONAL ANESTHETICS
Mimimum Alveolar Concentration (MAC)
-dose required to eliminate painful response in 50% of Px
Most Potent: methoxyflurane
Least Potent: Nitrous Oxide
a. Nitrous Oxide
b. Desflurane
c. Sevoflurane
d. Isoflurane
e. Halothane
f. Enflurane
2. INTRAVENOUS ANESTHETIC
a. Thiopental
b. Midazolam
c. Ketamine
d. Etomidate
e. Fentanyl, Morphine
f. Propofol
II. LOCAL ANESTHETICS
a. Esters
b. Amide