Antidote for human

1. A M R I T P O K H R E L
P H A R M A C I S T
Analgesic, Antidotes,
Anticholinergics and
Anticoagulants

2. Analgesic Dugs
 An analgesic or Painkiller is any member of the
group of drugs used to achieve analgesia-relief from
pain.
 Major classes of analgesic Drugs include
1. Opioids Groups
2. NSAIDs Groups

3. Narcotic Analgesic/Opioids
 Narcotic analgesic are drugs that relieve pain, by
binding to opioid receptor which are present in the
central and peripheral nervous system, can cause
numbness and induce a state of unconsciousness.
It includes:
 1. Natural: Morphine, Codeine
 2. Synthetic Derivatives: Fentanyl, Pethidine,
Tramadol

4. Morphine
Morphine is the major analgesic drug contained in crude
opium and is the prototype strong agonist.
 It may be given by IV, IM, o by mouth often as slow
release tablets.
Action of Morphine:
 Analgesia
 Euphoria and Sedation
 Respiratory depression and suppression of cough
 Nausea and Vomiting
 Histamine release causing bronchoconstiction
 Reduce gastric motility causing constipation

5. Disadvantage
Drug of addiction due to euphoric effect
Over dose cause poisoining; Respiatory depression
and coma
Cause dryness of mouth, mental clouding, vomiting,
headache, fatigue, costipation

6. Fentanyl
It is highly potent synthetic derivative with action
similar to those of morphine but with a more rapid
onset and shorter duration of action.
 The main use is in anaesthesia and chronic pain
management.
 Fentanyl can be used in infusion for severe pain
management where short duration of action is
desired.
 Fentanyl Patches are also available which are
advantageous for long term management of chronic
pain.

7. Opioids Antagonist
These drugs produce very little effect when given on
their own but block the effect of opiates.
 The most important example are:
Naloxone
Naltrexone

8. Naloxone
 It was the first pure opioid antagonist with affinity
for all opioids receptor
 The main clinical use of Naloxone are
To treat respiratory depression caused by opiate over
dosage. It is given intravenously and its effects are
produced immediately

9. summary
Drugs Uses Adverse Effects
Morphine Widely used for acute and
chronic pain
Sedation, Respiatory
Depression, Tolerance,
Dependence, Euphoria
Pethidine Acute Pain management As morphine ,
anticholinergic effects
Pentazocine Mainly acute pain May precipitate morphine
withdrawal syndrome
Fentanyl Acute pain, Anaesthesia As morphine
Codeine Mild pain, Dry cough Mainly constipation
Tramadol Acute(Post operative),
and chronic pain
Dizziness

10. NSAIDS
These are for acute pain management
 Diclofenac: 50 mg every 8 hours
 Ibuprofen: It is dosed 400 mg every 4 to 6 hours.
 Naproxen: 250 to 500 mg every 12 hours
 Ketorolac is used to relieve moderately severe pain,
usually after surgery.
 paracetamol: Mild to moderate pain, moderate to
severe pain (as adjunctive therapy to opioids), and
temporary reduction of fever.

12. Antidotes

14. Classification of Antidotes
Depending on their action:
A. Chemical Antidotes: change the chemical
nature of poison.
For example, sodium thiosulphate which changes toxic
cyanide to the non-toxic thiocyanate; sodium
calcium edetate chelates agents used for heavy
metal poison.

15. B. Physiological Antidotes:
acts by producing the effect opposite to that of poison.
Naloxone against morphine overdose
N-Acetylcystine in paracetamol Poisoning

16. C. Mechanical Antidotes:
They prevent the absorption of poison into the body.
For example, activated charcoal adsorbs the
poison prior to absorption across intestinal wall

17. Therapeutic Uses
Antidotes are used in treatment of poisoning as well as
in case of over dose of drugs.

18. S.N
.
Poison/Drugs Antidotes Doses
1 Paracetamol
(acetaminophen)
(N-acetylcysteine) later
2 Anticoagulants, (
Warfarin)
(Vitamin K)
3 Anticoagulants, (
Heparin)
(Protamine) 1mg neutralize 90-115U
Heparin, Initial Dose
1mg/min to total dose
200mg in 2Hrs
4 Benzodiazepines (Flumazenil) Initial Dose 0.1-0.2mg IV
over 30-60Sec, repeat
0.1-0.2mg IV every min
5 Methanol (Ethanol or Fomepizole)

20. 6 Organophosphates a. Atropine
b. Pralidoxime
a. I.D- 0.5-2.0mg IV, repeat
every 3-5 minute until sweat
and secretion clears
b. I.D- 1gm IV over 15min then
IV infusion of 3-4mg/kg/hr
for 24-72hrs or until clinical
toxicity resolves
7 Opioids (Naloxone) I.D . 0.1-2.0mg IV
Opioid dependent patients
should receive 0.1mg IV every
30-60 Sec until clinical response
8 Atropine (Physostigmine) I.D. 0.5mg-2.0mg slow IV over
3-5 Min

22. Anticholinergic Drugs
Are agents that blocks the neurotransmitter
Acetylcholine in the CNS and PNS.
S.N Organ/System Response
1 Eye Mydriasis(Dilatation of Pupil) , Cycloplegia
2 Respiratory Tract Drying the Secretion(Mouth, Nose, Throat,
Bronchi)
Relaxation of Smooth muscle of bronchi
3 GI Decrease Secretion as well as motility
4 CVS Increase Pulse rate

23. Example
 Atropine
 Dicyclomine
 Glycopyrrolate
 Ipratropium
 Tiotropium

24. Uses
 Excessive vagal-induced bradycardia
 Diarrhoea
 Motion sickness
 Muscle spasms
 Chronic obstructive pulmonary disease (COPD)
 Asthma
 As Preanaesthetic Medication

25. Side Effects
 Blurred vision
 Dry mouth
 Dry eyes
 Decreased urine production
 Decreased sweat production
 Constipation
 Memory impairment
 Delirium
 Confusion

26. Anticoagulant Drugs

27. Anticoagulants
Clotting Process
Formation of a blood clot(thrombus) in blood vessel or
the heart.
May be life saving(when it plugs a several vessel) or life
threatening if it occludes vessel supplying a vital
structure.
The potential consequence is ischemic necrosis of cell
and tissue is known as infraction.
CVA(stroke), MI and PE are example are examples of
disorders resulting from thrombosis and embolism

28. Anticoagulants
 Drugs that help to prevent clotting of blood.
 They inhibit the chemical process of fibrin polymer
 These include heparin, Low molecular weight
heparin, Warfarin, etc.
Antiplatelets agents:
Molecule that do not allow platelet to aggregate and
thus prevent clotting especially in the arteries are
called antiplatelets drugs.
These include aspirin, Clopidogrel, Cilastazole.

29. USFDA Approved Indications

30. Anticoagulants
1. Used in vivo
a. Oral
b. Parenteral
2. Used in Vitro
a. Heparin
b. Calcium complexing agents
Sodium citrate
Sodium edetate
Sodium oxalate

32. Parenteral Anticoagulants
 Heparin
 Enoxaparin
 Daltaprin
 Fondaparinux
Oral Anticoagulants
Warfarin
Dabigatran
Rivaroxaban
Apaxiban

33. Heparin
Indications: Deep venous thrombosis(DVT),
pulmonary embolism, Initial management of
patients with unstable angina, acute myocardial
infarction, during and after coronary angioplasty or
stent placement and during surgery requiring
cardiopulmonary bypass, hemodialysis.
Side Effects: Hemorrhage, heparin-induced
thrombocytopenia (HIT), alopecia, bleeding and
osteoporosis
Can Only be administered by parenteral route.
Note: Need dosing schedule by aPTT monitoring

34. Enoxaparin
 Enoxaparin belongs to a class of drugs known as “low
molecular weight heparin” (LMWH), which is different
than heparin.
 It is used to prevent blood clots in the leg in patients who
are on bed rest or who are having hip replacement, knee
replacement, or stomach surgery. It is used in
combination with aspirin to prevent complications from
angina (chest pain) and heart attacks.
 It can be used in pregnant women at risk of thrombosis
and pregnancy complications. The main indications
are prophylaxis of venous thromboembolism and
prevention of pregnancy loss in thrombophilic women.

35. Warfarin
It is an oral anticoagulant drugs and is avilable in Tablet of 1mg, 2
mg, 3mg and 5 mg strength.
Indications:
 DVT and PE
 MI
 Unstable Angina
 RHD, Atrial fibrilation
 Cerebrovascular disease
 Vascular sugery,prosthetic heart valves,
side-effects
Haemorrhage, hypersensitivity, rash, alopecia, diarrhoea,
unexplained drop in haematocrit, ‘purple toes, jaundice, hepatic
dysfunction; also nausea, vomiting, and pancreatitis
Note:-Need dose adjustment by monitoring PT/INR regularly

38. Newer oral Anticoagulant
 Dabigatran, Rivaroxaban, Apixaban
Mainly indicated for DVT and PE.
Advantages:
No laboratory monitoring required
Lower risk of bleeding
Fewer drug interactions
Antithrombotic efficacy equal to warfarin.

39. The End