►►►►CLASS 1 A
QUINIDINE
DIARRHEA 24%
Cinchonism is most often a sign of chronic quinidine toxicity, but it may appear in sensitive patients after a single moderate dose.
PROCAINAMIDE
Hypotension and serious disturbances of cardiorhythm such as ventricular asystole or fibrillation are more common with intravenous administration of PA than with intramuscular administration. Because PA is a peripheral vasodilator in concentrations higher than the usual therapeutic range, transient high plasma levels which may occur especially during intravenous administration may produce temporary but at times severe lowering of blood pressure
DISOPYRAMIDE
The most serious adverse reactions are hypotension and congestive heart failure. The most common adverse reactions, which are dose dependent, are associated with the anticholinergic properties of the drug. These may be transitory, but may be persistent or can be severe. Urinary retention is the most serious anticholinergic effect.
Anticholinergic:
dry mouth (32%),
urinary hesitancy (14%),
constipation (11%)
►►►►CLASS 1B
LIDOCAINE
lidocaine for spinal anesthesia, the incidences of adverse reactions were reported to be about 3 percent each for positional headaches, hypotension and backache; 2 percent for shivering; and less than 1 percent each for peripheral nerve symptoms, nausea, respiratory inadequacy and double vision.
Toxicity is usually associated with serum lidocaine concentrations of 9 to 10 mcg per mL, but may occur with concentrations as low as 5 mcg/mL. Central nervous system toxicity has been observed in patients with hepatic cirrhosis who were receiving lidocaine at infusion rates as low as 2.2 to 2.5 mg per min.
MEXILETINE
NAUSEA /VOMITING/HEART BURN- 39.6%
DIZZINESS/LIGHT HEADEDNESS-26%
NON MUTAGENIC
PHENYTOIN
CNS USE The most notable signs of toxicity associated with the intravenous use of this drug are cardiovascular collapse and/or central nervous system depression. Hypotension does occur when the drug is administered rapidly by the intravenous route. The rate of administration is very important; it should not exceed 50 mg per minute in adults, and 1-3 mg/kg/min (or 50 mg per minute, whichever is slower) in pediatric patients.
The most common side effects are neurotoxic and dose-related. They include:
sedation
impaired memory
slurred speech
nystagmus
decreased coordination
confusion
dizziness
headache
Long-term side effects
Some other side effects only appear after a person has been using Dilantin for a number of months or years. They are usually related to taking high doses. The most common ones affect appearance:
overgrowth of the gums
excessive hair on the face or body
acne
coarseness of facial features
Overgrowth of the gums (gingival hyperplasia) is more common in children than in adults.
Urogenital:peyronies disease
skin : Dermatological manifestations sometimes accompanied by fever have included scarlatiniform or morbilliform rashes. A morbilliform rash (measles-like) is the most common; other types of dermatitis are seen more rarely
The lethal dose in adults is estimated to be 2 to 5 grams. The initial symptoms are nystagmus, ataxia, and dysarthria. Other signs are tremor, hyperreflexia, lethargy, slurred speech, nausea, vomiting. The patient may become comatose and hypotensive. Death is due to respiratory and circulatory depression.
There are marked variations among individuals with respect to phenytoin plasma levels where toxicity may occur.
►Nystagmus, on lateral gaze, usually appears at 20 mcg/mL,
►ataxia at 30 mcg/mL;
►dysarthria and lethargy appear when the plasma concentration is over 40 mcg/mL, but as high a concentration as 50 mcg/mL has been reported without evidence of toxicity. As much as 25 times the therapeutic dose has been taken to result in a serum concentration over 100 mcg/mL with complete recovery.
TOCAINAMIDE
paranoid psychosis-NOT USED
►►►►CLASS 1C
ENCAINIDE - NOT USED NOW
PRO arrythimic effects
FLECAINIDE
Dizziness 18%
Visual Disturbances 15%
Dyspnea 10%
(Dizziness includes reports of dizziness, lightheadedness, faintness, unsteadiness, near syncope, etc.
Visual disturbance includes reports of blurred vision, difficulty in focusing, spots before eyes, etc.)
Flecainide, like other antiarrhythmic agents, can cause new or worsened supraventricular or ventricular arrhythmias. Ventricular proarrhythmic effects range from an increase in frequency of PVCs to the development of more severe ventricular tachycardia, e.g., tachycardia that is more sustained or more resistant to conversion to sinus rhythm, with potentially fatal consequences.
In studies of ventricular arrhythmia patients treated with flecainide, three-fourths of proarrhythmic events were new or worsened ventricular tachyarrhythmias, the remainder being increased frequency of PVCs ornewsupraventricular arrhythmias.
♣In patients treated with flecainide for sustained ventricular tachycardia, 80% (51/64) of proarrhythmic events occurred within 14 days of the onset of therapy.
Flecainide slows cardiac conduction in most patients to produce dose-related increases in PR, QRS, and QT intervals. PR interval increases on average about 25% (0.04 seconds) and as much as 118% in some patients. Approximately one-third of patients may develop new first-degree AV heart block (PR interval ≥ 0.2 seconds).
The QRS complex increases on average about 25% (0.02 seconds) and as much as 150% in some patients. Many patients develop QRS complexes with a duration of 12 seconds or more.
In one study, 4% of patients developed new bundle branch block while on flecainide.
The degree of lengthening of PR and QRS intervals does not predict either efficacy or the development of cardiac adverse effects.
In clinical trials, it was unusual for PR intervals to increase to 0.3 seconds or more, or for QRS intervals to increase to 18 seconds or more.
Thus, caution should be used when such intervals occur, and dose reductions may be considered.
The QT interval widens about 8%, but most of this widening (about 60% to 90%) is due to widening of the QRS duration.
PROPAFENONE
Unusual Taste
Nausea Vomiting
Dizziness
Elevated ANA Titers
Positive ANA titers have been reported in patients receiving propafenone
Agranulocytosis (fever, chills, weakness, and neutropenia) has been reported in patients receiving propafenone. Generally, the agranulocytosis occurred within the first two months of propafenone therapy and upon discontinuation of therapy, the white count usually normalized by 14 days. Unexplained fever and/or decrease in white cell count, particularly during the initial three months of therapy, warrant consideration of possible agranulocytosis/granulocytopenia. Patients should be instructed to promptly report the development of any signs of infection such as fever, sore throat, or chills.
Overall in clinical trials with propafenone, 4.7% of all patients had new or worsened ventricular arrhythmia possibly representing a proarrhythmic event (0.7% was an increase in PVCs; 4.0% a worsening, or new appearance, of VT or VF).
MORICIZINE
The most serious adverse reaction reported for is proarrhythmia
Most common : Dizziness 11% Nausea 7%
ADENOSINE
Many individuals experience facial flushing, a temporary rash on the chest, lightheadedness, diaphoresis, or nausea after administration of adenosine due to its vasodilatory effects.
►Metallic taste is a hallmark side-effect of adenosine administration. These symptoms are transitory, usually lasting less than one minute.
►It is classically associated with a sense of "impending doom", more prosaically described as apprehension. This lasts a few seconds after administration of a bolus dose, during transient asystole induced by intravenous administration. In some cases, adenosine can make patients' limbs feel numb for about 2–5 minutes after administration intravenously depending on the dosage (usually above 12 mg).
Metabolism
S/E after IV
Flushing 44%
Chest discomfort 40%
Dyspnea or urge to breathe deeplY 28%
Headache 18%
Throat, neck or jaw discomfort 15%
Gastrointestinal discomfort 13%
Lightheadedness/dizziness 12%
QUINIDINE
DIARRHEA 24%
Cinchonism is most often a sign of chronic quinidine toxicity, but it may appear in sensitive patients after a single moderate dose.
PROCAINAMIDE
Hypotension and serious disturbances of cardiorhythm such as ventricular asystole or fibrillation are more common with intravenous administration of PA than with intramuscular administration. Because PA is a peripheral vasodilator in concentrations higher than the usual therapeutic range, transient high plasma levels which may occur especially during intravenous administration may produce temporary but at times severe lowering of blood pressure
DISOPYRAMIDE
The most serious adverse reactions are hypotension and congestive heart failure. The most common adverse reactions, which are dose dependent, are associated with the anticholinergic properties of the drug. These may be transitory, but may be persistent or can be severe. Urinary retention is the most serious anticholinergic effect.
Anticholinergic:
dry mouth (32%),
urinary hesitancy (14%),
constipation (11%)
►►►►CLASS 1B
LIDOCAINE
lidocaine for spinal anesthesia, the incidences of adverse reactions were reported to be about 3 percent each for positional headaches, hypotension and backache; 2 percent for shivering; and less than 1 percent each for peripheral nerve symptoms, nausea, respiratory inadequacy and double vision.
Toxicity is usually associated with serum lidocaine concentrations of 9 to 10 mcg per mL, but may occur with concentrations as low as 5 mcg/mL. Central nervous system toxicity has been observed in patients with hepatic cirrhosis who were receiving lidocaine at infusion rates as low as 2.2 to 2.5 mg per min.
MEXILETINE
NAUSEA /VOMITING/HEART BURN- 39.6%
DIZZINESS/LIGHT HEADEDNESS-26%
NON MUTAGENIC
PHENYTOIN
CNS USE The most notable signs of toxicity associated with the intravenous use of this drug are cardiovascular collapse and/or central nervous system depression. Hypotension does occur when the drug is administered rapidly by the intravenous route. The rate of administration is very important; it should not exceed 50 mg per minute in adults, and 1-3 mg/kg/min (or 50 mg per minute, whichever is slower) in pediatric patients.
The most common side effects are neurotoxic and dose-related. They include:
sedation
impaired memory
slurred speech
nystagmus
decreased coordination
confusion
dizziness
headache
Long-term side effects
Some other side effects only appear after a person has been using Dilantin for a number of months or years. They are usually related to taking high doses. The most common ones affect appearance:
overgrowth of the gums
excessive hair on the face or body
acne
coarseness of facial features
Overgrowth of the gums (gingival hyperplasia) is more common in children than in adults.
Urogenital:peyronies disease
skin : Dermatological manifestations sometimes accompanied by fever have included scarlatiniform or morbilliform rashes. A morbilliform rash (measles-like) is the most common; other types of dermatitis are seen more rarely
The lethal dose in adults is estimated to be 2 to 5 grams. The initial symptoms are nystagmus, ataxia, and dysarthria. Other signs are tremor, hyperreflexia, lethargy, slurred speech, nausea, vomiting. The patient may become comatose and hypotensive. Death is due to respiratory and circulatory depression.
There are marked variations among individuals with respect to phenytoin plasma levels where toxicity may occur.
►Nystagmus, on lateral gaze, usually appears at 20 mcg/mL,
►ataxia at 30 mcg/mL;
►dysarthria and lethargy appear when the plasma concentration is over 40 mcg/mL, but as high a concentration as 50 mcg/mL has been reported without evidence of toxicity. As much as 25 times the therapeutic dose has been taken to result in a serum concentration over 100 mcg/mL with complete recovery.
TOCAINAMIDE
paranoid psychosis-NOT USED
►►►►CLASS 1C
ENCAINIDE - NOT USED NOW
PRO arrythimic effects
FLECAINIDE
Dizziness 18%
Visual Disturbances 15%
Dyspnea 10%
(Dizziness includes reports of dizziness, lightheadedness, faintness, unsteadiness, near syncope, etc.
Visual disturbance includes reports of blurred vision, difficulty in focusing, spots before eyes, etc.)
Flecainide, like other antiarrhythmic agents, can cause new or worsened supraventricular or ventricular arrhythmias. Ventricular proarrhythmic effects range from an increase in frequency of PVCs to the development of more severe ventricular tachycardia, e.g., tachycardia that is more sustained or more resistant to conversion to sinus rhythm, with potentially fatal consequences.
In studies of ventricular arrhythmia patients treated with flecainide, three-fourths of proarrhythmic events were new or worsened ventricular tachyarrhythmias, the remainder being increased frequency of PVCs ornewsupraventricular arrhythmias.
♣In patients treated with flecainide for sustained ventricular tachycardia, 80% (51/64) of proarrhythmic events occurred within 14 days of the onset of therapy.
Flecainide slows cardiac conduction in most patients to produce dose-related increases in PR, QRS, and QT intervals. PR interval increases on average about 25% (0.04 seconds) and as much as 118% in some patients. Approximately one-third of patients may develop new first-degree AV heart block (PR interval ≥ 0.2 seconds).
The QRS complex increases on average about 25% (0.02 seconds) and as much as 150% in some patients. Many patients develop QRS complexes with a duration of 12 seconds or more.
In one study, 4% of patients developed new bundle branch block while on flecainide.
The degree of lengthening of PR and QRS intervals does not predict either efficacy or the development of cardiac adverse effects.
In clinical trials, it was unusual for PR intervals to increase to 0.3 seconds or more, or for QRS intervals to increase to 18 seconds or more.
Thus, caution should be used when such intervals occur, and dose reductions may be considered.
The QT interval widens about 8%, but most of this widening (about 60% to 90%) is due to widening of the QRS duration.
PROPAFENONE
Unusual Taste
Nausea Vomiting
Dizziness
Elevated ANA Titers
Positive ANA titers have been reported in patients receiving propafenone
Agranulocytosis (fever, chills, weakness, and neutropenia) has been reported in patients receiving propafenone. Generally, the agranulocytosis occurred within the first two months of propafenone therapy and upon discontinuation of therapy, the white count usually normalized by 14 days. Unexplained fever and/or decrease in white cell count, particularly during the initial three months of therapy, warrant consideration of possible agranulocytosis/granulocytopenia. Patients should be instructed to promptly report the development of any signs of infection such as fever, sore throat, or chills.
Overall in clinical trials with propafenone, 4.7% of all patients had new or worsened ventricular arrhythmia possibly representing a proarrhythmic event (0.7% was an increase in PVCs; 4.0% a worsening, or new appearance, of VT or VF).
MORICIZINE
The most serious adverse reaction reported for is proarrhythmia
Most common : Dizziness 11% Nausea 7%
ADENOSINE
Many individuals experience facial flushing, a temporary rash on the chest, lightheadedness, diaphoresis, or nausea after administration of adenosine due to its vasodilatory effects.
►Metallic taste is a hallmark side-effect of adenosine administration. These symptoms are transitory, usually lasting less than one minute.
►It is classically associated with a sense of "impending doom", more prosaically described as apprehension. This lasts a few seconds after administration of a bolus dose, during transient asystole induced by intravenous administration. In some cases, adenosine can make patients' limbs feel numb for about 2–5 minutes after administration intravenously depending on the dosage (usually above 12 mg).
Metabolism
S/E after IV
Flushing 44%
Chest discomfort 40%
Dyspnea or urge to breathe deeplY 28%
Headache 18%
Throat, neck or jaw discomfort 15%
Gastrointestinal discomfort 13%
Lightheadedness/dizziness 12%
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