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Tranq,sed,hypnotic

pharmacology

QuestionAnswer
Agents- depress central nervous system which enables the animal to go to sleep more easily. e.g. Chloral Hydrate. Hypnotic
Drugs which relives anxiety and results in - easer for patient to rest or sleep. Sedative
These drugs causes drowsiness. Sedative
Xylazine is more like sedative
Predominant action of these drugs is in relieving anxiety without producing undue sleep. They affect mood and behavior Tranquilizer (Ataractic)
Some times these three categories are classified, based on medical-clinical uses. Antianxiety: (older terminology “ Neuroleptics”) Antipsychotic: Sedative/ Hypnotic
Drugs which reduce psychomotor agitation, curiosity, and aggressiveness exert their effects by blocking dopamine mediated responses in the central nervous system (CNS
Phenothiazine and Butyrophenone.. they are now categorized as antipsychotic drugs.
are used for premedication but they will not quieten the animal and may be more difficult to handle by removing inhibition. So that the vicious animal become more likely to bite or kick. Benzodiazepines:
Classification Phenothiazines. II. Butyrophenone. III. Benzodiazepines.IV. Alpha-2- Adrenoceptor Agonist.V. Analgesic drugs. (i). NonsteroidsVI. Opioid Analgesics
Phenothiazine Tranquilizers Acepromazine.Promazine.ChlorpromazinePropriopromazine.Triflupromazine.MethotrimeprazinePromethazine
They are dopamine antagonist, having calming and mood altering effects. They can increase the rate of turnover (synthesis and destruction) in the brain. They also increase turnover of norepinephrine Phenothiazine Tranquilizers
This group is classified as antipsychotic agent and have wide range of central and peripheral effects., but the degree of activity varies Phenothiazine Tranquilizers
Powerful antiemetic. Phenothiazine Tranquilizers
In general they do not have analgesic activity. Phenothiazine Tranquilizers
Alpha-1-adrenoceptor blocker, can cause hypotension Phenothiazine Derivatives
Has antiarrhythmic effect on heart Phenothiazine Derivatives
Has spasmolytic action on the gut, in horse gut motility is not reduced Phenothiazine Derivatives
Varying degree of antihistamine activity. Phenothiazine Derivatives
May cause hypothermia: It acts on CNS thermoregulation center to drop body temperature Phenothiazine Derivatives
FDA approved for dog, cat and horse. Acepromazine
Can be given, I/V, I/M and subcutaneous Acepromazine
Oral doses can also be used Acepromazine
Possesses antiemetic, anticonvulsant, antispasmodic, hypotension and hypothermic properties Acepromazine
Lowers the convulsive seizure threshold thus contraindicated seizure cases Acepromazine
May prevent malignant hyperthermia syndrome in susceptible pig exposed to halothane Acepromazine
Decreases PCV Acepromazine
Not to use with organophosphate compounds, may cause seizure activity Acepromazine
In horse it may cause priapism, thus not to use in stallion Acepromazine
In halothane anesthesia, epinephrine induced ventricular arrhythmias and fibrillation can be prevented Acepromazine
Increase doses does not increase tranquilization. May even cause excitement Acepromazine
Widely used in Europe Propionylpromazine
Less potent than acepromazine. Had unreliable action in horses. Mostly used in human subjects. Chlorpromazine
Action similar to acepromazine. Has better sedative effect than chlorpromazine Promazine
Is a typical phenothiazine but it is also a potent analgesic, having a potency about 0.7 times that of morphine Methotrimeprazine
Is mostly used as antihistamine Promethazine
Butyrophenone Derivatives Azaperone, Droperidol and Fluanisone
class of drugs causes tranquilization and sedation, anti-emetics, reduce motor activity and inhibits CNS catecholamines (dopamine, norepinephrine). butyrophenone
Not marketed in USA Azaperone
Mostly used in pigs in other countries. Azaperone
Has been effective in halothane induced malignant hyperthermia in susceptible pigs Azaperone
. Its effects can be antagonized by 4-aminopyridine. Duration of action 2 to 3 hours. Azaperone
Used for control of aggressiveness when mixing or regrouping the pigs. Metabolized by liver Azaperone
Is along acting (6-8 hours), potent neuroleptic. Its use is approved in dogs. Droperidol
The principal use has been as a compound of Innovar-Vet in mixture with fentanyl. This combination produces neuroleptic-analgesia Droperidol
Was used in 70’s and 80’s, but no longer marketed Droperidol
This combination produces neuroleptic-analgesia compound of Innovar-Vet in mixture with fentanyl
These agent are used for their central (CNS) effect of profound sedation and analgesia Alpha-2 Adrenergic Agonists
CNS depression is mediated by stimulation (activation) of alpha-2-adrenoceptrs Alpha-2 Adrenergic Agonists
Even at sub-sedative doses, analgesia occurs through both spinal and central action Alpha-2 Adrenergic Agonists
share similar regions of the brain Opioid and Alpha-2-adrenoceptors
The locus ceruleus (located in ventral medulla) in brain is believed to be the major site of action for alpha-2-sedatives.
Alpha-2-adernergic Agonist Sedation: Primary action is mediated by activation of alpha-2-adrenoceptors They serve as prejunctional inhibitory receptors (autorecptor) with in the sympathetic nervous system.
Alpha-2-adernergic Agonist Muscle relaxant activity is caused by/ inhibition of intraneural transmission with in CNS system
Alpha-2-adernergic Agonist CNS effects: Anticonvulsant and also may be effective in cases of opioid withdrawal syndrome.
Alpha-2-adrenoceptors Agonist Systemic Effects: GI tract, uterus, kidney, platelets and verity of other effects
Alpha-2-adrenoceptors Agonist Peripheral Effects: Hypertension: Post-synaptic alpha-1 and -2. Hypotension: Mediated via CNS causing decreased sympathetic out flow by activation of pre-synaptic alpha-2
Alpha-2-adrenoceptors Agonist Cardio-Pulmonary effects: A-V block, decrease heart rate by enhancing vagal tone. pulmonary effect: Depress respiratory center in medulla etc..
Alpha-2-adenoceptors Agonists: Xylazine.Detomidine.Medetomine.Romifidine
Alpha-2-adenoceptors Antagonists: YohimbineTolazolineIodazoxan.Atipamezole
Is approved by FDA for dog, cat and horse. Not approved for ruminants Xylazine
Can be used in combination with other drugs. Xylazine
Half life; Sheep = 23 min., Dog = 30 min. Cattle =36 min., and horse =50 min Xylazine
Duration of action: 15-30 min. Also dose dependent Xylazine
Can be given IV, IM, S/C. Xylazine
Cattle more sensitive than other animals Xylazine
Cardio-vascular and respiratory depression. HR , CO, BP, Resp Xylazine
Horse may respond with well directed kick (Kick response) due to sudden touch. Xylazine
Horse: Violent excitement (IV), sudden death and collapse. May be intra-carotid injection Xylazine
Vomiting in dog and cat Xylazine
Hyperglycemia. Xylazine
Urine production increases. Anti-ADH effect. Xylazine
Uterine contraction: May cause abortion in cow in last trimester of pregnancy Xylazine
May cause anaphylactic shock Xylazine
Used as premedication for sedation and analgesia. Xylazine
Can be used for epidural anesthesia. Xylazine
Xylazine Metabolized by liver and excreted by kidney
Xylazine Precaution and Contraindications; Heart condition,Liver and renal impairment,Can cause hypothermia in cold temperature,May also cause hyperthermia in hot summer in Alabama due to depression of respiratory center,causing decreased respiration,Shock and dehydration.Epilepsy.
Developed for horses and cattle Detomidine (Dormosedan)
Has higher potency and greater specificity at central alpha-2-adrenoceptros Detomidine (Dormosedan)
Cardiovascular effects similar to xylazine. Detomidine (Dormosedan)
Sedation last for 90 to 120 min. Detomidine (Dormosedan)
Pain relief for 75 to 80 min. Used in equine colic cases. Detomidine (Dormosedan)
Do NOT have ecbolic effect in cattle Detomidine (Dormosedan)
Other effects are similar to xylazine Detomidine (Dormosedan)
Is most potent alpha-2-adrenoceptor agent. Medetomidine
Sedation, analgesia, muscle relaxation occurs in variety of domestic animals Medetomidine
Selectivity binding ratio for: alpha-2 / alpha-1.Medetomidine Detomidine Clonidine Xylazine 1620, 260, 220, 160
In dogs and cats it produces. Dose dependent sedation and analgesia Medetomidine
Where as with xylazine and detomidine, higher doses may not result in more sedation, but increase in duration of action. Medetomidine
Drug is used as premedication before induction of anesthesia .. In combination with other drugs Medetomidine
Horse: Produces more ataxia and disorientation, thus not preferred Medetomidine
Primarily used in dog and cats Medetomidine
Contra indications are: Similar to xylazine and other drugs in this group Medetomidine
Pharmacokinetics: Onset of action is rapid (5min) with IV and 10 to 15 min with IM injections Medetomidine
Drug not recommended for use in pregnant dogs Medetomidine
It is safe to use with opioids, Benz diazepam and other anesthetics Medetomidine
This drug, developed from clonidine, has typical alpha-2-adrenoceptor against effect Romifidine
Used thus far in horses as sedative and premedication Romifidine
Produces less ataxia and head in not lowered at the same extent Romifidine
Duration of action is longer than the others Romifidine
Horse remains quieter than normal for considerable time after obvious sedation has waned. Causes marked urination in about 90 min. Romifidine
Maximal Sedative IV doses in horse are: Romifidine Xylazine Detomidine Romifidine 80 ug/kgXylazine 1mg/kgDetomidine 20 ug/kg.
Alpha-2-Adrenoceptor Antagonists are Yohimbine.Iodazoxan.Tolazoline.Atipamezole
is not Alpha-2- Adrenoceptor antagonists, but causes release of acetylcholine and other neurotransmitters from CNS pre-synaptic nerve endings. Thus has been used to reverse the action of some the alpha-2- agonists *** 4-aminopyridine
Is very effective alpha-2-antagonists Yohimbine
It reverses sedation and analgesia in many animal species Yohimbine
Is a Rauwolfia or indolealkylamine of alkaloid. It is chemically related to reserpine Yohimbine
Action is alpha-2 adrenoceptor mediated depression (blocking central alpha-2 receptors) thus enhance norepinephrine release and increase sympathetic out flow Yohimbine
It penetrate CNS quite readily, reversal of xylazine occurs in 3 min Yohimbine
Alpha-adrenergic blocker and structurally related to phentolamine Tolazoline (Priscoline)
Possesses the least specificity for alpha-2-adrenoceptor than all other antagonists in this group Tolazoline (Priscoline)
Is approved for xylazine reversal in horse. Tolazoline (Priscoline)
Given IV rapid action is in 5 min Tolazoline (Priscoline)
It is also a competitive alpha 1 and alpha 2 adrenergic blocker, thus has peripheral vasodilation Tolazoline (Priscoline)
Anti-sedative effect is far superior than other drugs in this group Atipamezole
Alpha 2/ alpha 1, selective ratio of atipamezole is 200 to 300 times higher than idazoxan or yohimbine. Atipamezole
Is an alpha 2- adrenergic antagonist Atipamezole
Its labeled for use as medetomidine reversal agent. Atipamezole
Some animal have died following rapid IV of high doses Atipamezole
Not recommended in pregnant and lactating animal Atipamezole
a purine alkyl piperidine derivative has been used in clinical investigation in cattle for its sedative effects Tameridone
Has been tried for the capture and transport of wild ruminants Tameridone
It’s a sedative drugs but details NOT known Tameridone
Created by: alljacks