Pleno Pakar

061115

Pc4 Blok Fam Med

Dr.Datten Bangun
MSc,SpFK
Dept.Farmakologi &
Therapeutik
Fak.Kedokteran USU
 Introduction
What is a drug?
Traditionally, a drug is a therapeutic
chemical designed to have maximal benefits
with minimal risks of side effects or toxicity.
What is a psychoactive drug?
A Drug that can change cognition, behavior
and emotions by changing the functioning
of the brain.
Some psychoactive drugs:
Caffeine, heroin, alcohol, Prozac
 Menurut BNN
Ada 12.044 orang meninggal tiap
tahun akibat Narkoba di Indonesia .
( Koran Analisa Medan. 5 November
2015)
 Drug Use
Definitions
Taking a psychoactive substance for non-medical
purposes, out of curiosity
Drug Abuse
Drug use that leads to problems (e.g. loss of
effectiveness in society; behavioral
psychopathology, criminal acts)
Drug Dependence
A maladaptive pattern of drug use leading to clinically-
significant impairment or distress, associated with difficulty
in controlling drug-taking behavior, withdrawal, and
tolerance
The state of needing a drug to function within normal limits
 Nature of Addiction - a
continuum of use?

Loss of control

However, addiction is more than mere dr

 How are drugs
classified?:
According to the physiological effect
they have
Stimulants, speed up the central nervous
system(CNS).
Depressants, slow down the CNS
Psychoactive drugs alter feelings
Narcotics, are powerful painkillers
Designer drugs try to mimic narcotics or
other drugs:amphetamines,
hallucinogens.
Halucinogenics
 Controlled Substances
Controlled substances are drugs or other
substances that are controlled under the
Controlled Substances Act (CSA).
This act categorizes all substances which are
regulated under federal law into schedules,
depending on how hazardous they are.
The schedule the drug is placed under
depends on its medical use, its potential for
abuse, and its safety or how easily people
become dependent on it.
 Schedule I controlled substances
Schedule I substances are those that have the
following findings:
The drug or other substance has a high potential for abuse.
The drug or other substance has no currently accepted
medical use in treatment in the United States.
There is a lack of accepted safety for use of the drug or
other substance under medical supervision
= Cathinone, an amphetamine-like stimulant found in the
shrub Catha edulis (khat
= heroin; LSD (lysergic acid diethylamide);MDMA ("ecstasy"),
 Schedule II substances
Schedule II substances are those that have the
following findings:
The drug or other substances have a high
potential for abuse
The drug or other substances have currently
accepted medical use in treatment in the
United States, or currently accepted medical
use with severe restrictions
Abuse of the drug or other substances may lead
to severe psychological or physical
dependence.[
 Drugs in this schedule II
include:
Cocaine (used as a topical anesthetic)
Amphetamine (originally placed in Schedule III, but moved to
Schedule II in 1971), Adderall, Dextroamphetamine
(Dexedrine), Lisdexamfetamine (Vyvanse): treatment of ADHD,
narcolepsy
Methylphenidate (Ritalin, Concerta), Dexmethylphenidate
(Focalin): treatment of ADHD, narcolepsy
Methamphetamine: treatment of ADHD, severe obesity
Opium, opium tincture (Laudanum): treatment as a potent
antidiarrheal
Fentanyl and most other strong pure opioid agonists, i.e.
levorphanol, opium
Methadone: treatment of heroin addiction, extreme chronic
pain
 Schedule III controlled
substances
Schedule III substances are those that have
the following findings:
The drug or other substance has a potential
for abuse less than the drugs or other
substances in schedules I and II.
The drug or other substance has a currently
accepted medical use in treatment in the
United States.
Abuse of the drug or other substance may
lead to moderate or low physical dependence
or high psychological dependence
 Schedule III controlled
substances
Drugs in this schedule include:
Anabolic steroids (including prohormones
such as androstenedione)
Intermediate-acting barbiturates, such as
talbutal or butalbital; Buprenorphine (semi-
synthetic opioid; active in Suboxone,
Subutex) Dihydrocodeine when
compounded with other substances, to a
certain dosage and concentration. Ketamine
 Schedule IV controlled
substances
Schedule IV substances are those that have
the following findings:
The drug or other substance has a low
potential for abuse relative to the drugs or
other substances in schedule III
The drug or other substance has a currently
accepted medical use in treatment in the
United States
Abuse of the drug or other substance may
lead to limited physical dependence or
psychological dependence relative to the
drugs or other substances in schedule II
 What is drug abuse?
How do drugs of addiction
work?
Most drugs of abuse mimi

Kriteria Ketergantungan Obat:

---- DSM IV--------- Dept.Psikiatri
Most psychoactive drugs of abuse look
similar to neurotransmitters.
These drugs mimic the action and
appearance of neurotransitters.
= THC Anandamide

= Opiates Endorphin Enkephalin

= Alcohol, Benzos, Barbs GABA
= Stimulants - catecholamines
 Drugs of Abuse are
Dopaminergic
Or, in other words, they increase dopamine
activity.

EXAMPLE:
THC connects
with receptors
and causes the
release of
dopamine
DopaminePathways

striatum

frontal hippocampus
cortex

substantia
nigra/VTA
Functions
reward(motivation) SerotoninPathw
nucleus
pleasure,euphoria accumbens
motorfunction Functions
(finetuning) raphe mood
compulsion memory
perserveration processing
decisionmaking
sleep
 vesicle
stimulation Drug : Neuronal terminal
cocaine transporter
ritalin
Vmat

/serotonin

DA/5HT
How some drugs of abuse cause dopamine release:
opioids narcotics (activate opioid receptors)
nicotine (activate nicotine receptors)
marijuana (activate cannabinoid receptors)
caffeine
alcohol (activate GABA receptors; an inhibitory transmitter)
 transporter

Vmat serotonin/

ReleaseDAfromvesiclesandreverse
transporter
DA/5HT

DrugTypes:
Amphetamines
methamphetamine
MDMA(Ecstasy)
 Natural Rewards Elevate Dopamine Levels

FOOD SEX

DA Concentration (% Baseline)
200 200
NAc shell
% of Basal DA Output

150 150

Copulation Frequency
100 100
15

Empty 10
50
Box Feeding
5

0 0
0 60 120 180 ScrScr Scr Scr
BasFemale 1 Present Female 2 Present
Time (min) Sample1 2 3 4 5 6 7 8 9 1011121314151617
Number
Mounts
Intromissions
Ejaculations

Source: Di Chiara et al. Source: Fiorino and Phillips

 Effects of drugs on dopamine level
Accumbens AMPHETAMINE COCAINE
% of Basal Release

1100 Accumbens

% of Basal Release
1000 400
900
800 DA
DA 300 DOPAC
700 DOPAC HVA
600 HVA
500 200
400
300
200 100
100
0
0 1 2 3 4 5 hr 0
0 1 2 3 4 5 hr
Time After Amphetamine Time After Cocaine

MORPHINE
% of Basal Release

% of Basal Release
250
NICOTINE 250 Accumbens
Dose
200 (mg/kg)
0.5
Accumbens 200
Caudate 1.0
2.5
150 150 10

100 100

0 0
0 1 2 3 hr 0 1 2 3 4 5hr
Time After Nicotine Time After Morphine
Source: Di Chiara and Imperato
 The Reward System
The Reward System is theneural
network involved in feelingpleasure.
Its also centrally involved in learning
and motivation.
The primaryneurotransmitter inthe
Reward System isdopamine.
If enough dopamine is released into
the brains reward circuits,euphoria
results.
 The Reward System
Dopamine-based exhilaration is a
common experience, at least
partially responsible just about
anytime one experiences pleasure.
A hug, a kiss, a word of praise or
a winning poker hand,or
achievement in sport,dancing can
trigger a dopamine spike
andpleasure
 Brain Reward system
Addictive drugs produce a high
by overstimulating the brains
Reward System.To explain more
fully, some background
abouthow the brainworks is
necessary.
 Substances that can be
abused
There are four characteristics of drugs that
are
frequently abused:
1.The drug creates an altered state of
consciousness---- euphoria
2.Prolonged use of the drug creates a
tolerance for the drug
3.The desirable effect is quick
4.Withdrawal symptoms develop if the drug
is stopped after prolonged use.

Administration of the agonist drug is a fast w

to treat withdrawal symptoms
WHO ABUSE DRUGS?
Those who abuse drugs do so because
They are:
= bored
= pressured by their peers
= affluent and want to experiment
= seeking to escape reality
= feeling inadequate
= feeling ashamed and depressed
= seeking relief from conflicts

Dont forget: Genetic factors==== jangan coba-

coba,
You never know what genetic factors you have
Genetics

Gene/
Environment
Interaction

Environment
 CLUB DRUGS

Ecstasy
(methylenedioxymethamphetamine)
GHB (Gamma-hydroxybutyrate)
Rohypnol (Flunitrazepam related to
Valium, Xanax)
Ketamine ( anesthetic for humans and
animals, injected, smoked)
Methamphetamine
LSD (Lysergic Acid Diethylamide 25)
 CLUB DRUGS
Ecstasy Deve.
In 1900 as appetite suppressant.
Has effects of Stimulant and
Hallucinogen, effects last approx 3-6hrs.
Usual side effects (confusion, depression,
sleep problems, anxiety, paranoia,
dehydration, hypertension and heart or
kidney failure) can last up to 1 mo.
Significant increase in BP, heart rate,
increased sense of alertness and energy.
 CLUB DRUGS
Rohypnol In the benzodiazepine family (valium, xanax).
Is tasteless and odorless, dissolves easily in carbonated
beverages.
Effects are aggravated by concurrent use of alcohol. Even
without alcohol, a dose of Rohypnol can impair a victim for 8 to
12 hours..

The drug causes profound anterograde amnesia;, individuals

may not remember events experienced while under the
influence.

==== Advice for girls:

======= Never leave your drinks unattended

One of the street names is the forget-me-pill, and has/is

used in many reported/unreported sexual assaults.
 What is khat
The World Health Organization (WHO)
lists khat as a drug that creates
dependence in people, meaning it
produces a continuing desire to keep using
it.
Khat contains stimulants similar to
amphetamines
In Somalia, civilian and military use of
khat has been blamed for fueling civil
war, draining the nation's economy, and
undermining international relief efforts.
Legal Status

- Cathinone- Schedule I Final Action

2/93
- Produces a euphoric effect
similar to amphetamine in that it
stimulates the Central nervous system
- Begins to degrade 48 hours
after harvesting
- Proper handling can prolong
potency
Structural Similarities
Cathinone Cathine
O OH

NH2 NH2

Amphetamine Methamphetamine

NH2 NHCH3
 Bath salts?Khat
Bath salts are usually ingested by
= sniffing or snorting it when in powder form.
=They can also be taken orally, smoked, or put
into a solution and injected into veins.
Reported Effects of Bath Salts Use
Agitation
Combative behavior
Hallucinations
Paranoia
Confusion
Anxiety
Involuntary muscle movements
Khat
 Why Cant Addicts Just Quit?
Non-Addicted Brain Addicted Brain

Control
Control

Saliency Drive NO Saliency Drive GO

GO

Memory Memory

Because Addiction Changes Brain Circuits

Source: Adapted from Volkow et al., Neuropharmacology, 2004.
This is why addicts cant just quit

This is why treatment is essential

 Treating a Biobehavioral Disorder Must Go
Beyond Just Fixing the Chemistry
We Need to Treat the
Whole Person!

Pharmacological
Behavioral Therapies
(medications)

Medical and Social Services

In Social Context
Thank you